Binding Database

PubMed Identification:

Starting with __ _1 _2 _3 _4 _5 _6 _7 _8 _9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34

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10999999

Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.

J Med Chem 43: 3453-73 (2000)

COR Therapeutics Inc

2D 3D TSV

10999489

2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes.

Bioorg Med Chem Lett 10: 2141-4 (2000)

University of Amsterdam

2D 3D TSV

10999488

7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.

Bioorg Med Chem Lett 10: 2137-40 (2000)

Celltech-Chiroscience Ltd

2D 3D TSV

10999484

Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: a novel series of mixed dopamine D2/D4 receptor antagonists.

Bioorg Med Chem Lett 10: 2119-22 (2000)

Neurogen Corporation

2D 3D TSV

10999482

Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.

Bioorg Med Chem Lett 10: 2111-4 (2000)

Merck Research Laboratories

2D 3D TSV

10999477

Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.

Bioorg Med Chem Lett 10: 2087-90 (2000)

Kyoto University

2D 3D TSV

10999475

Naphthalene carboxamides as inhibitors of human cytomegalovirus DNA polymerase.

Bioorg Med Chem Lett 10: 2079-81 (2000)

Pharmacia

2D 3D TSV

10999473

Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.

Bioorg Med Chem Lett 10: 2071-4 (2000)

Institute

2D 3D TSV

10999472

Computational binding studies of human pp60c-src SH2 domain with a series of nonpeptide, phosphophenyl-containing ligands.

Bioorg Med Chem Lett 10: 2067-70 (2000)

Yale University

2D 3D TSV

10999471

A novel inhibitor of human telomerase derived from 10H-indolo[3,2-b]quinoline.

Bioorg Med Chem Lett 10: 2063-6 (2000)

Reading University

2D 3D TSV

10999468

1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.

Bioorg Med Chem Lett 10: 2051-4 (2000)

Bayer Research Center

2D 3D TSV

10999467

Discovery of a new class of p38 kinase inhibitors.

Bioorg Med Chem Lett 10: 2047-50 (2000)

Bayer Research Center

2D 3D TSV

10998351

Specificity and mechanism of action of some commonly used protein kinase inhibitors.

Biochem J 351: 95-105 (2001)

University of Dundee

2D 3D TSV

10998059

Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25.

Eur J Biochem 267: 5983-94 (2000)

CNRS

2D 3D TSV

168

10997946

Selective inhibition of human cytochrome P450 3A4 by N-[2(R)-hydroxy-1(S)-indanyl]-5-[2(S)-(1, 1-dimethylethylaminocarbonyl)-4-[(furo[2, 3-b]pyridin-5-yl)methyl]piperazin-1-yl]-4(S)-hydroxy-2(R)-phenylmethy lpentanamide and P-glycoprotein by valspodar in gene transfectant systems.

Drug Metab Dispos 28: 1238-43 (2000)

University of Tokyo

2D 3D TSV

10991999

Characterization of the anxiolytic properties of a novel neuroactive steroid, Co 2-6749 (GMA-839; WAY-141839; 3alpha, 21-dihydroxy-3beta-trifluoromethyl-19-nor-5beta-pregnan-20-one), a selective modulator of gamma-aminobutyric acid(A) receptors.

J Pharmacol Exp Ther 295: 337-45 (2000)

CoCensys Inc

2D 3D TSV

10991998

Cannabinoid agonist signal transduction in rat brain: comparison of cannabinoid agonists in receptor binding, G-protein activation, and adenylyl cyclase inhibition.

J Pharmacol Exp Ther 295: 328-36 (2000)

Wake Forest University

2D 3D TSV

10991988

Interaction and transport of thiazide diuretics, loop diuretics, and acetazolamide via rat renal organic anion transporter rOAT1.

J Pharmacol Exp Ther 295: 261-5 (2000)

Kyoto University Hospital

2D 3D TSV

10991983

Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.

J Pharmacol Exp Ther 295: 226-32 (2000)

Albany Medical College

2D 3D TSV

10991954

Nonsteroidal anti-inflammatory drugs efficiently reduce the transport and cytotoxicity of adefovir mediated by the human renal organic anion transporter 1.

J Pharmacol Exp Ther 295: 10-5 (2000)

Gilead Sciences Inc

2D 3D TSV

10987445

Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.

Bioorg Med Chem Lett 10: 2041-4 (2001)

Friedrich-Alexander University

2D 3D TSV

140

10987444

Design and synthesis of potent thiol-based inhibitors of endothelin converting enzyme-1.

Bioorg Med Chem Lett 10: 2037-9 (2001)

Novartis Institute for BioMedical Research

2D 3D TSV

10987441

Use of proline bioisosteres in potential HIV protease inhibitors: phenylalanine-2-thiophenoxy-3-pyrrolidinone: synthesis and anti-HIV evaluation.

Bioorg Med Chem Lett 10: 2023-6 (2001)

Université de la Méditerranée

2D 3D TSV

10987435

Synthesis and erythropoietin receptor binding affinities of N,N-disubstituted amino acids.

Bioorg Med Chem Lett 10: 1995-9 (2001)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10987434

Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines.

Bioorg Med Chem Lett 10: 1991-4 (2001)

Wyeth-Ayerst Research

2D 3D TSV

10987430

Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.

Bioorg Med Chem Lett 10: 1975-8 (2001)

Merck Research Laboratories

2D 3D TSV

10987429

Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.

Bioorg Med Chem Lett 10: 1971-3 (2001)

Merck Research Laboratories

2D 3D TSV

10987424

The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. Part 1.

Bioorg Med Chem Lett 10: 1949-52 (2001)

AstraZeneca Pharmaceuticals

2D 3D TSV

10987423

Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.

Bioorg Med Chem Lett 10: 1943-8 (2001)

Merck Research Laboratories

2D 3D TSV

10987417

Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists.

Bioorg Med Chem Lett 10: 1917-20 (2001)

Merck Research Laboratories

2D 3D TSV

10987415

Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase.

Bioorg Med Chem Lett 10: 1909-11 (2001)

University of Canterbury

2D 3D TSV

10980448

Human liver glycogen phosphorylase inhibitors bind at a new allosteric site.

Chem Biol 7: 677-82 (2000)

Pfizer Inc

2D 3D TSV

10978197

Workup-dependent formation of 5-lipoxygenase inhibitory boswellic acid analogues.

J Nat Prod 63: 1058-61 (2000)

Institute of Pharmaceutical Sciences

2D 3D TSV

10978192

Privileged molecules for protein binding identified from NMR-based screening.

J Med Chem 43: 3443-7 (2000)

Abbott Laboratories

2D 3D TSV

10978189

Structure-activity studies including a Psi(CH(2)-NH) scan of peptide YY (PYY) active site, PYY(22-36), for interaction with rat intestinal PYY receptors: development of analogues with potent in vivo activity in the intestine.

J Med Chem 43: 3420-7 (2000)

University of Cincinnati Medical Center

2D 3D TSV

115

10978188

Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines.

J Med Chem 43: 3408-19 (2000)

CoCensys Inc

2D 3D TSV

10978187

Synthesis and biological activity of a novel 11a-homo (cyclohexyl) prostaglandin.

J Med Chem 43: 3400-7 (2000)

Alcon Laboratories Inc

2D 3D TSV

10978186

Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.

J Med Chem 43: 3386-99 (2000)

Merck Research Laboratories

2D 3D TSV

10978184

Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a dual Na(+) and Ca(2+) channel blocker with antioxidant activity.

J Med Chem 43: 3372-6 (2000)

Suntory Biomedical Research Limited

2D 3D TSV

10978183

Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery.

J Med Chem 43: 3351-71 (2000)

BASF Bioresearch Corporation

2D 3D TSV

10974196

Biochemical and cellular effects of c-Src kinase-selective pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.

Biochem Pharmacol 60: 885-98 (2000)

Parke-Davis Pharmaceutical Research

2D 3D TSV

10973807

Molecular identification of a rat novel organic anion transporter moat1, which transports prostaglandin D(2), leukotriene C(4), and taurocholate.

Biochem Biophys Res Commun 275: 831-8 (2000)

Tohoku University School of Medicine

2D 3D TSV

10969992

Arylsulfonyl-N,N-diethyl-dithiocarbamates: a novel class of antitumor agents.

Bioorg Med Chem Lett 10: 1887-91 (2000)

Università degli Studi

2D 3D TSV

10969990

Synthesis and HIV-1 integrase inhibitory activities of caffeoylglucosides.

Bioorg Med Chem Lett 10: 1879-82 (2000)

Institute of Science and Technology

2D 3D TSV

10969989

Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist.

Bioorg Med Chem Lett 10: 1875-8 (2000)

Shionogi & Co., Ltd

2D 3D TSV

10969988

Aminoalkyl adenylate and aminoacyl sulfamate intermediate analogues differing greatly in affinity for their cognate Staphylococcus aureus aminoacyl tRNA synthetases.

Bioorg Med Chem Lett 10: 1871-4 (2000)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10969987

1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists.

Bioorg Med Chem Lett 10: 1867-70 (2000)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10969986

1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.

Bioorg Med Chem Lett 10: 1863-6 (2000)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

123

10969978

A solid-phase synthesis for beta-turn mimetics of sialyl Lewis X.

Bioorg Med Chem Lett 10: 1827-30 (2000)

Nippon Organon K.K.

2D 3D TSV

10969976

Cinnamaldehydes inhibit cyclin dependent kinase 4/cyclin D1.

Bioorg Med Chem Lett 10: 1819-22 (2000)

Korea Research Institute of Bioscience and Biotechnology

2D 3D TSV

10969974

Inhibitors of bacterial tyrosyl tRNA synthetase: synthesis of four stereoisomeric analogues of the natural product SB-219383.

Bioorg Med Chem Lett 10: 1811-4 (2000)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10969973

4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.

Bioorg Med Chem Lett 10: 1807-10 (2000)

Eli Lilly and Company

2D 3D TSV

103

10969972

CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound.

Bioorg Med Chem Lett 10: 1803-6 (2000)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10969967

Synthesis and monoamine transporter affinity of 2beta-carbomethoxy-3beta-(2''-, 3''- or 4''-substituted) biphenyltropanes.

Bioorg Med Chem Lett 10: 1783-5 (2000)

Yale University

2D 3D TSV

10966924

Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney.

Am J Physiol Renal Physiol 279: 449-58 (2000)

Medical College of Georgia

2D 3D TSV

10966754

3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group.

J Med Chem 43: 3348-50 (2000)

University of Bristol

2D 3D TSV

10966753

Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile as a high-affinity nonsteroidal androgen receptor ligand.

J Med Chem 43: 3344-7 (2000)

The University of Michigan Medical School

2D 3D TSV

10966752

New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.

J Med Chem 43: 3335-43 (2000)

Freie Universität Berlin

2D 3D TSV

10966747

Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects.

J Med Chem 43: 3283-94 (2000)

Georgetown University Medical Center

2D 3D TSV

10966743

4-Anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor kinase and their bioisosteric relationship to the 4-anilino-6,7-dialkoxyquinazoline inhibitors.

J Med Chem 43: 3244-56 (2000)

Wyeth-Ayerst Research

2D 3D TSV

10966742

GRid-INdependent descriptors (GRIND): a novel class of alignment-independent three-dimensional molecular descriptors.

J Med Chem 43: 3233-43 (2000)

University of Perugia

2D 3D TSV

10966741

Crystal structures of human factor Xa complexed with potent inhibitors.

J Med Chem 43: 3226-32 (2000)

Aventis Pharma

2D 3D TSV

10966739

Conformationally constrained analogues of diacylglycerol (DAG). 17. Contrast between sn-1 and sn-2 DAG lactones in binding to protein kinase C.

J Med Chem 43: 3209-17 (2000)

National Cancer Institute-Bethesda

2D 3D TSV

10964567

Structural basis for isotype selectivity of the human retinoic acid nuclear receptor.

J Mol Biol 302: 155-70 (2000)

CNRS

2D 3D TSV

10963748

The suramin analogue NF279 is a novel and potent antagonist selective for the P2X(1) receptor.

Neuropharmacology 39: 2044-53 (2000)

University of Frankfurt

2D 3D TSV

10956228

Probes for narcotic receptor-mediated phenomena. 27. Synthesis and pharmacological evaluation of selective delta-opioid receptor agonists from 4-[(alphaR)-alpha-(2S,5R)-4-substituted-2, 5-dimethyl-1-piperazinyl-3-methoxybenzyl]-N,N-diethylbenzamides and their enantiomers.

J Med Chem 43: 3193-6 (2000)

National Institute of Diabetes and Digestive and Kidney Diseases

2D 3D TSV

10956225

Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents.

J Med Chem 43: 3168-85 (2000)

Pfizer Inc

2D 3D TSV

106

10956223

Use of an additional hydrophobic binding site, the Z site, in the rational drug design of a new class of stronger trypanothione reductase inhibitor, quaternary alkylammonium phenothiazines.

J Med Chem 43: 3148-56 (2000)

University of Manchester

2D 3D TSV

10956222

Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src).

J Med Chem 43: 3134-47 (2000)

University of Auckland

2D 3D TSV

105

10956221

Effect of C9-methyl substitution and C8-C9 conformational restriction on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.

J Med Chem 43: 3125-33 (2000)

Duquesne University

2D 3D TSV

10956220

Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.

J Med Chem 43: 3118-24 (2000)

Universita' di Firenze

2D 3D TSV

10956219

Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.

J Med Chem 43: 3111-7 (2000)

Bristol-Myers Squibb Pharmaceutical Research Institute

2D 3D TSV

10956218

Novel radiotracers for imaging the serotonin transporter by positron emission tomography: synthesis, radiosynthesis, and in vitro and ex vivo evaluation of (11)C-labeled 2-(phenylthio)araalkylamines.

J Med Chem 43: 3103-10 (2000)

Centre for Addiction and Mental Health

2D 3D TSV

10956215

1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT(2A) partial agonists.

J Med Chem 43: 3074-84 (2000)

Virginia Commonwealth University

2D 3D TSV

10956212

3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth.

J Med Chem 43: 3045-51 (2000)

Georgetown University Medical Center

2D 3D TSV

10956211

GRID/CPCA: a new computational tool to design selective ligands.

J Med Chem 43: 3033-44 (2000)

Boehringer Ingelheim Pharma KG

2D 3D TSV

10956210

DoMCoSAR: a novel approach for establishing the docking mode that is consistent with the structure-activity relationship. Application to HIV-1 protease inhibitors and VEGF receptor tyrosine kinase inhibitors.

J Med Chem 43: 3020-32 (2000)

Eli Lilly and Company

2D 3D TSV

10956209

CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors.

J Med Chem 43: 3005-19 (2000)

University of Texas

2D 3D TSV

10956208

Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists.

J Med Chem 43: 2992-3004 (2000)

University of Catania

2D 3D TSV

121

10956207

2-Carbomethoxy-3-aryl-8-bicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters.

J Med Chem 43: 2982-91 (2000)

Organix Inc

2D 3D TSV

10956205

Identification of a chemical tool for the orphan nuclear receptor FXR.

J Med Chem 43: 2971-4 (2000)

Glaxo Wellcome Research & Development

2D 3D TSV

10956202

Synthesis and evaluation of peptidomimetics as selective inhibitors and active site probes of nitric oxide synthases.

J Med Chem 43: 2938-45 (2000)

Northwestern University

2D 3D TSV

10956198

Permanently charged chiral 1,4-dihydropyridines: molecular probes of L-type calcium channels. Synthesis and pharmacological characterization of methyl(omega-trimethylalkylammonium) 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate iodide, calcium channel antagonists.

J Med Chem 43: 2906-14 (2000)

State University of New York

2D 3D TSV

10956197

Adenosine kinase inhibitors. 2. Synthesis, enzyme inhibition, and antiseizure activity of diaryltubercidin analogues.

J Med Chem 43: 2894-905 (2000)

Metabasis Therapeutics Inc

2D 3D TSV

10956196

Adenosine kinase inhibitors. 1. Synthesis, enzyme inhibition, and antiseizure activity of 5-iodotubercidin analogues.

J Med Chem 43: 2883-93 (2000)

Metabasis Therapeutics Inc

2D 3D TSV

10956195

Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907).

J Med Chem 43: 2871-82 (2000)

University Centre for Pharmacy

2D 3D TSV

10956194

Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors.

J Med Chem 43: 2860-70 (2000)

Vanderbilt University School of Medicine

2D 3D TSV

152

10956192

Synthesis of novel 5-substituted 3-amino-3,4-dihydro-2H-1-benzopyran derivatives and their interactions with the 5-HT1A receptor.

J Med Chem 43: 2837-50 (2000)

AstraZeneca R&D Södertälje

2D 3D TSV

10956191

Design and synthesis of potent hexapeptide and heptapeptide gonadotropin-releasing hormone antagonists by truncation of a decapeptide analogue sequence.

J Med Chem 43: 2831-6 (2000)

Institute of Science

2D 3D TSV

10956190

Structure-activity studies of reduced-size gonadotropin-releasing hormone agonists derived from the sequence of an endothelin antagonist.

J Med Chem 43: 2824-30 (2000)

Institute of Science

2D 3D TSV

10956189

A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives.

J Med Chem 43: 2814-23 (2000)

Universit£ di Pisa

2D 3D TSV

10956188

Further studies on nociceptin-related peptides: discovery of a new chemical template with antagonist activity on the nociceptin receptor.

J Med Chem 43: 2805-13 (2000)

University of Ferrara

2D 3D TSV

10956187

Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.

J Med Chem 43: 2797-804 (2000)

University of Newcastle

2D 3D TSV

10956186

A refined 3-dimensional QSAR of cytochrome P450 2C9: computational predictions of drug interactions.

J Med Chem 43: 2789-96 (2000)

Washington State University

2D 3D TSV

10956183

De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.

J Med Chem 43: 2775-8 (2000)

Synaptic Pharmaceutical Corporation

2D 3D TSV

10945872

Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.

J Pharmacol Exp Ther 294: 1154-65 (2000)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10944518

The first selective agonist for the neuropeptide YY5 receptor increases food intake in rats.

J Biol Chem 275: 36043-8 (2000)

Federal Institute of Technology of Zurich

2D 3D TSV

10937745

Development of peptidyl alpha-keto-beta-aldehydes as new inhibitors of cathepsin L--comparisons of potency and selectivity profiles with cathepsin B.

Bioorg Med Chem Lett 10: 1771-3 (2000)

Queen's University Belfast

2D 3D TSV

10937743

Grignard-mediated synthesis and preliminary biological evaluation of novel 3-substituted farnesyl diphosphate analogues.

Bioorg Med Chem Lett 10: 1763-6 (2000)

Wayne State University

2D 3D TSV

10937738

Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors.

Bioorg Med Chem Lett 10: 1745-8 (2000)

University of Barcelona

2D 3D TSV

10937736

Nonbenzamidine compounds as selective factor Xa inhibitors.

Bioorg Med Chem Lett 10: 1737-9 (2000)

Aventis Pharmaceuticals, Inc.

2D 3D TSV

10937734

Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.

Bioorg Med Chem Lett 10: 1729-31 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10937733

Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents.

Bioorg Med Chem Lett 10: 1723-7 (2000)

Merck Research Laboratories

2D 3D TSV

10937732

6-Bicyclopiperazinyl-1-arylsulfonylindoles and 6-bicyclopiperidinyl-1-arylsulfonylindoles derivatives as novel, potent, and selective 5-HT6 receptor antagonists.

Bioorg Med Chem Lett 10: 1719-21 (2000)

NPS Allelix Corp.

2D 3D TSV

10937729

5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.

Bioorg Med Chem Lett 10: 1707-9 (2000)

NPS Allelix Corp.

2D 3D TSV

10937725

Anhydride modified cantharidin analogues: synthesis, inhibition of protein phosphatases 1 and 2A and anticancer activity.

Bioorg Med Chem Lett 10: 1687-90 (2000)

The University of Newcastle

2D 3D TSV

10937724

Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors.

Bioorg Med Chem Lett 10: 1681-6 (2000)

Georgetown University Medical Center

2D 3D TSV

10937721

Inhibition of dopamine receptors by endogenous amines: binding to striatal receptors and pharmacological effects on locomotor activity.

Bioorg Med Chem Lett 10: 1669-71 (2000)

University of Tokyo

2D 3D TSV

10937720

Combined tachykinin receptor antagonist: synthesis and stereochemical structure-activity relationships of novel morpholine analogues.

Bioorg Med Chem Lett 10: 1665-8 (2000)

Sankyo Co., Ltd

2D 3D TSV

10937715

Novel inhibitors of AP-1 and NF-kappaB mediated gene expression: structure-activity relationship studies of ethyl 4-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-2-(trifluoromethyl)++ +pyrimidi ne-5-carboxylate.

Bioorg Med Chem Lett 10: 1645-8 (2000)

Signal Pharmaceuticals, Inc.

2D 3D TSV

10937714

N-acylated alpha-(3-pyridylmethyl)-beta-aminotetralin antagoinists of the human neuropeptide Y Y5 receptor.

Bioorg Med Chem Lett 10: 1641-3 (2000)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10937713

Solid-phase synthesis of an arylsulfone hydroxamate library.

Bioorg Med Chem Lett 10: 1637-40 (2000)

Rhone-Poulenc Rorer

2D 3D TSV

186

10937710

Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.

Bioorg Med Chem Lett 10: 1625-8 (2000)

Merck & Co.

2D 3D TSV

10937709

Phenylacetamides as selective alpha-1A adrenergic receptor antagonists.

Bioorg Med Chem Lett 10: 1621-4 (2000)

Merck & Co.

2D 3D TSV

10936213

Insect nicotinic acetylcholine receptor: conserved neonicotinoid specificity of [(3)H]imidacloprid binding site.

J Neurochem 75: 1294-303 (2000)

University of California

2D 3D TSV

10929807

Fluorescence-based assay for the interaction of small molecules with the human renal organic anion transporter 1.

Anal Biochem 283: 49-55 (2000)

Gilead Sciences

2D 3D TSV

10926521

Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design.

J Mol Biol 301: 465-75 (2000)

Max-Planck-Institut fuer Biochemie

2D 3D TSV

10915062

Michael adducts of ascorbic acid as inhibitors of protein phosphatase 2A and inducers of apoptosis.

Bioorg Med Chem Lett 10: 1605-8 (2000)

Universität Göttingen

2D 3D TSV

10915060

Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226.

Bioorg Med Chem Lett 10: 1597-600 (2000)

University of Regensburg

2D 3D TSV

10915056

Difluoroketones as inhibitors of matrix metalloprotease-13.

Bioorg Med Chem Lett 10: 1581-4 (2000)

Pfizer Inc

2D 3D TSV

10915054

Kinetic characterisation of ene-diol-based inhibitors of alpha-amylase.

Bioorg Med Chem Lett 10: 1575-6 (2000)

University of Canterbury

2D 3D TSV

10915052

The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors.

Bioorg Med Chem Lett 10: 1567-70 (2000)

Novartis Horsham Research Centre

2D 3D TSV

10915051

The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.

Bioorg Med Chem Lett 10: 1563-6 (2000)

Novartis Horsham Research Centre

2D 3D TSV

10915050

Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1.

Bioorg Med Chem Lett 10: 1559-62 (2000)

Inha University

2D 3D TSV

10915049

1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors.

Bioorg Med Chem Lett 10: 1555-8 (2000)

Novartis Institute for BioMedical Research

2D 3D TSV

10915044

Synthesis and PTP1B inhibition of novel 4-aryl-1-oxa-9-thiacyclopenta[b]fluorenes.

Bioorg Med Chem Lett 10: 1535-8 (2000)

Wyeth-Ayerst Research

2D 3D TSV

10915043

Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists.

Bioorg Med Chem Lett 10: 1531-4 (2000)

Merck Research Laboratories

2D 3D TSV

10915042

Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library.

Bioorg Med Chem Lett 10: 1527-30 (2000)

Merck Research Laboratories

2D 3D TSV

10915041

Synthesis of fluorescent probes directed to the active site gorge of acetylcholinesterase.

Bioorg Med Chem Lett 10: 1523-6 (2000)

The University of Montana

2D 3D TSV

10915040

Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues.

Bioorg Med Chem Lett 10: 1519-22 (2000)

Procter & Gamble Pharmaceuticals

2D 3D TSV

10915035

Cell adhesion antagonists: synthesis and evaluation of a novel series of phenylalanine based inhibitors.

Bioorg Med Chem Lett 10: 1497-9 (2000)

Millennium Pharmaceutical

2D 3D TSV

10908357

Recognition of a cognate RNA aptamer by neomycin B: quantitative evaluation of hydrogen bonding and electrostatic interactions.

Nucleic Acids Res 28: 2935-42 (2000)

The Ohio State University

2D 3D TSV

10903938

Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.

Chem Biol 7: 493-504 (2000)

Novartis Pharmaceuticals

2D 3D TSV

10901697

Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro.

Drug Metab Dispos 28: 895-8 (2000)

Vanderbilt University School of Medicine

2D 3D TSV

10900230

Agonist-directed trafficking of porcine alpha(2A)-adrenergic receptor signaling in Chinese hamster ovary cells: l-isoproterenol selectively activates G(s).

J Pharmacol Exp Ther 294: 539-47 (2000)

University of Michigan

2D 3D TSV

10893315

A rapid computational method for lead evolution: description and application to alpha(1)-adrenergic antagonists.

J Med Chem 43: 2770-4 (2000)

CombiChem, Inc.

2D 3D TSV

10893314

Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.

J Med Chem 43: 2759-69 (2000)

University of Minnesota

2D 3D TSV

10893311

Development of a lead inhibitor for the A16V+S108T mutant of dihydrofolate reductase from the cycloguanil-resistant strain (T9/94) of Plasmodium falciparum.

J Med Chem 43: 2738-44 (2000)

National Center for Genetic Engineering and Biotechnology at Thailand

2D 3D TSV

10893310

Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.

J Med Chem 43: 2731-7 (2000)

Arizona State University

2D 3D TSV

10893308

In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.

J Med Chem 43: 2703-18 (2000)

Merck Research Laboratories

2D 3D TSV

102

10893307

[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.

J Med Chem 43: 2698-702 (2000)

University of California

2D 3D TSV

10893306

Synthesis and pharmacological evaluation of new pyrazolidine-3, 5-diones as AT(1) angiotensin II receptor antagonists.

J Med Chem 43: 2685-97 (2000)

Université de Lille 2

2D 3D TSV

10893305

Synthesis and antitumor activity of new benzoheterocyclic derivatives of distamycin A.

J Med Chem 43: 2675-84 (2000)

Universit£ di Ferrara

2D 3D TSV

10893303

Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases.

J Med Chem 43: 2655-63 (2000)

SUGEN, Inc.

2D 3D TSV

100

10893301

Ligands for glutamate receptors: design and therapeutic prospects.

J Med Chem 43: 2609-45 (2000)

The Royal Danish School of Pharmacy

2D 3D TSV

270

10891120

Novel nonsubstrate inhibitors of human thymidine phosphorylase, a potential target for tumor-dependent angiogenesis.

J Med Chem 43: 2601-7 (2000)

Istituto di Genetica Biochimica ed Evoluzionistica

2D 3D TSV

10891118

Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability.

J Med Chem 43: 2586-90 (2000)

University of Northern Colorado

2D 3D TSV

10891114

Aureobasidins: structure-activity relationships for the inhibition of the human MDR1 P-glycoprotein ABC-transporter.

J Med Chem 43: 2547-56 (2000)

Strasbourg 1 University

2D 3D TSV

10891111

4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.

J Med Chem 43: 2523-9 (2000)

Eisai Company, Ltd

2D 3D TSV

10891110

6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.

J Med Chem 43: 2514-22 (2000)

National Institute of Diabetes and Digestive and Kidney Diseases

2D 3D TSV

10891109

Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.

J Med Chem 43: 2506-13 (2000)

Palacky University

2D 3D TSV

10891107

Reporter affinity labels: an o-phthalaldehyde derivative of beta-naltrexamine as a fluorogenic ligand for opioid receptors.

J Med Chem 43: 2489-92 (2000)

University of Minnesota

2D 3D TSV

10891096

Structure-based design and solid-phase parallel synthesis of phosphorylated nonpeptides to explore hydrophobic binding at the Src SH2 domain.

J Comb Chem 2: 305-13 (2000)

ARIAD Pharmaceuticals Inc

2D 3D TSV

10890171

Synthesis and biological activities of an alpha-methyl and a beta-methyl carbapenem and the corresponding unsubstituted compound.

Bioorg Med Chem Lett 10: 1389-91 (2000)

University of Munich

2D 3D TSV

10890169

N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.

Bioorg Med Chem Lett 10: 1381-4 (2000)

Merck Sharp & Dohme Research Laboratories

2D 3D TSV

10890168

Synthesis and resolution of racemic eliprodil and evaluation of the enantiomers of eliprodil as NMDA receptor antagonists.

Bioorg Med Chem Lett 10: 1377-80 (2000)

Zentrum für Pharmaforschung

2D 3D TSV

10890163

Convergent synthesis of ribonuclease L-active 2',5'-oligoadenylate-peptide nucleic acids.

Bioorg Med Chem Lett 10: 1357-60 (2000)

National Institute of Diabetes and Digestive antd Kidney Diseases

2D 3D TSV

10890162

Nonpeptide endothelin antagonists: from lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids.

Bioorg Med Chem Lett 10: 1351-5 (2000)

Hoechst Marion Roussel Inc

2D 3D TSV

10890161

Synthesis and uptake of nitric oxide-releasing drugs by the P2 nucleoside transporter in Trypanosoma equiperdum.

Bioorg Med Chem Lett 10: 1347-50 (2000)

Universit£ de Toulouse III

2D 3D TSV

10890154

Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor.

Bioorg Med Chem Lett 10: 1315-6 (2000)

Kitasato University

2D 3D TSV

10888340

Synthesis of N-diisopropyl phosphoryl benzyltetrahydroisoquinoline, a new class of mitochondrial complexes I and III inhibitors.

Bioorg Med Chem Lett 10: 1491-4 (2000)

Universidad de Valencia

2D 3D TSV

10888337

Potent new leucine aminopeptidase inhibitor of novel structure synthesised by a modified Wadsworth-Emmons (Horner) Wittig procedure.

Bioorg Med Chem Lett 10: 1481-2 (2000)

The Queen's University of Belfast

2D 3D TSV

10888335

Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.

Bioorg Med Chem Lett 10: 1471-5 (2000)

The Scripps Research Institute

2D 3D TSV

10888334

N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N-methyl-3,5-bis-trifluoromethyl-benzamide: an orally active neurokinin NK1/NK2 antagonist.

Bioorg Med Chem Lett 10: 1467-70 (2000)

Novartis Pharma AG

2D 3D TSV

10888332

Synthesis and structure-activity relationships of novel fungal chitin synthase inhibitors.

Bioorg Med Chem Lett 10: 1459-62 (2000)

Nippon Roche Research Center

2D 3D TSV

10888331

Natural and synthetic analogues of actinomycin D as Grb2-SH2 domain blockers.

Bioorg Med Chem Lett 10: 1455-7 (2000)

Korea Research Institute of Bioscience and Biotechnology

2D 3D TSV

10888329

Synthesis, molecular modeling and preliminary biological evaluation of 1-amino-3-phosphono-3-cyclopentene-1-carboxylic acid and 1-amino-3-phosphono-2-cyclopentene-1-carboxylic acid, two novel agonists of metabotropic glutamate receptors of group III.

Bioorg Med Chem Lett 10: 1447-50 (2000)

Università di Perugia

2D 3D TSV

10888328

An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes.

Bioorg Med Chem Lett 10: 1443-6 (2000)

Georgetown University Medical Center

2D 3D TSV

10888326

Synthesis of tetrakis(multifluoro-4-pyridyl)porphin derivatives as acetylcholinesterase inhibitors.

Bioorg Med Chem Lett 10: 1435-8 (2000)

Seoul National University

2D 3D TSV

10888325

Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.

Bioorg Med Chem Lett 10: 1431-4 (2000)

Merck Research Laboratories

2D 3D TSV

10888324

Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.

Bioorg Med Chem Lett 10: 1427-9 (2000)

Merck Research Laboratories

2D 3D TSV

10888319

Antifungal rapamycin analogues with reduced immunosuppressive activity.

Bioorg Med Chem Lett 10: 1405-8 (2000)

Abbott Laboratories

2D 3D TSV

10882376

A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography.

J Med Chem 43: 2479-83 (2000)

Rational Drug Design Laboratories

2D 3D TSV

10882373

6-N-Acyltriciribine analogues: structure-activity relationship between acyl carbon chain length and activity against HIV-1.

J Med Chem 43: 2457-63 (2000)

University of Michigan

2D 3D TSV

10882371

Deoxy sugar analogues of triciribine: correlation of antiviral and antiproliferative activity with intracellular phosphorylation.

J Med Chem 43: 2438-48 (2000)

University of Michigan

2D 3D TSV

10882369

Synthesis of B-ring homologated estradiol analogues that modulate tubulin polymerization and microtubule stability.

J Med Chem 43: 2419-29 (2000)

Purdue University

2D 3D TSV

10882365

A rational approach to the design and synthesis of a new bradykinin B(1) receptor antagonist.

J Med Chem 43: 2387-94 (2000)

University of Montpellier

2D 3D TSV

10882364

Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists.

J Med Chem 43: 2382-6 (2000)

University of Montpellier

2D 3D TSV

10882362

Design, synthesis, and structure-activity relationships of novel non-imidazole histamine H(3) receptor antagonists.

J Med Chem 43: 2362-70 (2000)

The James Black Foundation

2D 3D TSV

10882361

Synthesis and biological evaluation of bombesin constrained analogues.

J Med Chem 43: 2356-61 (2000)

University of Montpellier

2D 3D TSV

10882360

CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.

J Med Chem 43: 2350-5 (2000)

AstraZeneca R&D Boston

2D 3D TSV

10882359

17beta-O-Aminoalkyloximes of 5beta-androstane-3beta,14beta-diol with digitalis-like activity: synthesis, cardiotonic activity, structure-activity relationships, and molecular modeling of the Na(+),K(+)-ATPase receptor.

J Med Chem 43: 2332-49 (2000)

Prassis Istituto di Ricerche Sigma-Tau

2D 3D TSV

10882358

Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.

J Med Chem 43: 2324-31 (2000)

F. Hoffmann-La Roche Inc

2D 3D TSV

10882357

New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.

J Med Chem 43: 2310-23 (2000)

Novartis Pharmaceuticals

2D 3D TSV

10882356

A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.

J Med Chem 43: 2300-9 (2000)

Universit£ di Catania

2D 3D TSV

10882355

Fenchylamine sulfonamide inhibitors of amyloid beta peptide production by the gamma-secretase proteolytic pathway: potential small-molecule therapeutic agents for the treatment of Alzheimer's disease.

J Med Chem 43: 2297-9 (2000)

Amgen Inc

2D 3D TSV

10882354

Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold.

J Med Chem 43: 2293-6 (2000)

Pfizer Inc

2D 3D TSV

10882008

2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit.

Bioorg Med Chem 8: 957-75 (2000)

Alcon Research Ltd

2D 3D TSV

10882002

Cyclobutane carboxamide inhibitors of fungal melanin: biosynthesis and their evaluation as fungicides.

Bioorg Med Chem 8: 897-907 (2000)

Stine Haskell Research Center

2D 3D TSV

10869410

S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626.

J Pharmacol Exp Ther 293: 1048-62 (2000)

Centre de Recherches de Croissy

2D 3D TSV

10869408

Trans-stimulation effects of folic acid derivatives on methotrexate transport by rat renal organic anion transporter, OAT-K1.

J Pharmacol Exp Ther 293: 1034-9 (2000)

Kyoto University Hospital

2D 3D TSV

10869375

Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.

J Pharmacol Exp Ther 293: 771-8 (2000)

R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10869292

Rifamycin SV and rifampicin exhibit differential inhibition of the hepatic rat organic anion transporting polypeptides, Oatp1 and Oatp2.

Hepatology 32: 82-6 (2000)

University of Zurich

2D 3D TSV

10869205

The application of HPLC with on-line coupled UV/MS-biochemical detection for isolation of an acetylcholinesterase inhibitor from narcissus 'Sir Winston Churchill'.

J Nat Prod 63: 803-6 (2000)

Leiden University

2D 3D TSV

10869198

Antifungal substances against pathogenic fungi, talaroconvolutins, from talaromyces convolutus.

J Nat Prod 63: 768-72 (2000)

Hoshi University

2D 3D TSV

10869194

Inhibition of phospholipase cgamma1 and cancer cell proliferation by triterpene esters from Uncaria rhynchophylla.

J Nat Prod 63: 753-6 (2000)

Seoul National University

2D 3D TSV

10869191

Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species: novel inhibitors of protein kinases.

J Nat Prod 63: 739-45 (2000)

Heinrich-Heine-Universität

2D 3D TSV

10869183

Thermodynamics of sequence-specific binding of PNA to DNA.

Biochemistry 39: 7781-91 (2000)

Chalmers University of Technology

2D 3D TSV

10866404

Discovery of a potent, non-triketone type inhibitor of 4-hydroxyphenylpyruvate dioxygenase.

Bioorg Med Chem Lett 10: 1297-8 (2000)

Tunghai Christian University

2D 3D TSV

10866403

Total synthesis of pyrrolizidines 223H', 239K', 265H', and 267H' found in Madagascan frogs (Mantella) and their affinities for nicotinic acetylcholine receptor.

Bioorg Med Chem Lett 10: 1293-5 (2000)

Toyama Medical and Pharmaceutical University

2D 3D TSV

10866400

4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity.

Bioorg Med Chem Lett 10: 1281-4 (2000)

Research Triangle Institute

2D 3D TSV

10866399

Conformationally-restricted ligands for the histamine H1 receptor.

Bioorg Med Chem Lett 10: 1277-9 (2000)

University of Bath

2D 3D TSV

10866395

SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.

Bioorg Med Chem Lett 10: 1261-4 (2000)

Novartis Pharma AG

2D 3D TSV

10866394

Carbocyclic influenza neuraminidase inhibitors possessing a C3-cyclic amine side chain: synthesis and inhibitory activity.

Bioorg Med Chem Lett 10: 1257-60 (2000)

Gilead Sciences Inc

2D 3D TSV

10866393

Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.

Bioorg Med Chem Lett 10: 1253-6 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10866391

The design and synthesis of the high efficacy, non-peptide CCK1 receptor agonist PD170292.

Bioorg Med Chem Lett 10: 1245-8 (2000)

CCIPE-Faculte de Pharmacie

2D 3D TSV

10866390

(+)-4-phosphonophenylglycine (PPG) a new group III selective metabotropic glutamate receptor agonist.

Bioorg Med Chem Lett 10: 1241-4 (2000)

Novartis Pharma AG

2D 3D TSV

10866387

'Double-Drugs'--a new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker.

Bioorg Med Chem Lett 10: 1227-31 (2000)

Kyoto Pharmaceutical University

2D 3D TSV

10866385

Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.

Bioorg Med Chem Lett 10: 1219-21 (2000)

The Oxford Centre for Molecular Sciences

2D 3D TSV

10866377

Beta-casomorphins: substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity.

Bioorg Med Chem Lett 10: 1185-8 (2000)

Universit£ di Napoli Federico II

2D 3D TSV

10866375

Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists.

Bioorg Med Chem Lett 10: 1175-9 (2000)

Novartis Pharma AG

2D 3D TSV

10866374

The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic.

Bioorg Med Chem Lett 10: 1171-3 (2000)

Roche Research Center

2D 3D TSV

10866373

Cyclic thioether peptide mimetics as VCAM-VLA-4 antagonists.

Bioorg Med Chem Lett 10: 1167-9 (2000)

Roche Research Center

2D 3D TSV

10866372

Carbacyclic peptide mimetics as VCAM-VLA-4 antagonists.

Bioorg Med Chem Lett 10: 1163-5 (2000)

Roche Research Center

2D 3D TSV

10866371

Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.

Bioorg Med Chem Lett 10: 1159-62 (2000)

GlaxoSmithKline

2D 3D TSV

10854830

Inhibitory effect of anti-diabetic agents on rat organic anion transporter rOAT1.

Eur J Pharmacol 398: 193-7 (2000)

Kyoto University Hospital

2D 3D TSV

10854287

Behaviroal, pharmacological, and molecular characterization of an amphibian cannabinoid receptor.

J Neurochem 75: 413-23 (2000)

Oregon State University

2D 3D TSV

10853677

Discovery and evaluation of potent, tyrosine-based alpha4beta1 integrin antagonists.

Bioorg Med Chem Lett 10: 997-9 (2000)

Celltech Chiroscience

2D 3D TSV

10853676

Discovery and evaluation of potent, cysteine-based alpha4beta1 integrin antagonists.

Bioorg Med Chem Lett 10: 993-5 (2000)

Celltech Chiroscience

2D 3D TSV

10853674

Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors.

Bioorg Med Chem Lett 10: 983-7 (2000)

Corvas International Inc

2D 3D TSV

10853673

Beta-carbonyl substituted glutathione conjugates as inhibitors Of O. volvulus GST2.

Bioorg Med Chem Lett 10: 979-81 (2000)

University of Wales

2D 3D TSV

10853669

Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.

Bioorg Med Chem Lett 10: 963-6 (2000)

Berlex Biosciences

2D 3D TSV

102

10853668

Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.

Bioorg Med Chem Lett 10: 957-61 (2000)

Berlex Biosciences

2D 3D TSV

10853665

Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.

Bioorg Med Chem Lett 10: 945-9 (2000)

Novartis Pharma AG

2D 3D TSV

104

10853661

Examination of novel non-phosphorus-containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward Grb2 SH2 domains.

Bioorg Med Chem Lett 10: 923-7 (2000)

National Cancer Institute-Bethesda

2D 3D TSV

10853660

Pyrrolo[3,2,1-ij]quinoline derivatives, a 5-HT2c receptor agonist with selectivity over the 5-HT2a receptor: potential therapeutic applications for epilepsy and obesity.

Bioorg Med Chem Lett 10: 919-21 (2000)

NPS Allelix Corp.

2D 3D TSV

10853656

5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine.

Bioorg Med Chem Lett 10: 903-5 (2000)

NPS Allelix Corp.

2D 3D TSV

10853654

Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2.

Bioorg Med Chem Lett 10: 895-7 (2000)

Iowa State University

2D 3D TSV

10853650

Novel phenylpiperazine derivatives as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity.

Bioorg Med Chem Lett 10: 875-9 (2000)

Yoshitomi Pharmaceutical Industries Ltd

2D 3D TSV

10853647

Three-dimensional quantitative structure-activity relationship analyses of RGD mimetics as fibrinogen receptor antagonists.

Bioorg Med Chem Lett 10: 859-63 (2000)

Kyoto University

2D 3D TSV

10853646

The synthesis and evaluation of 3-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors.

Bioorg Med Chem Lett 10: 853-7 (2000)

Southern Methodist University

2D 3D TSV

10853645

The synthesis and evaluation of 2-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors.

Bioorg Med Chem Lett 10: 847-51 (2000)

Southern Methodist University

2D 3D TSV

10853644

SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.

Bioorg Med Chem Lett 10: 843-5 (2000)

Tunghai Christian University

2D 3D TSV

10851239

Characterization of the human cysteinyl leukotriene 2 receptor.

J Biol Chem 275: 30531-6 (2000)

University of Virginia

2D 3D TSV

10843593

Polyoxygenated dysidea sterols that inhibit the binding of [I125] IL-8 to the human recombinant IL-8 receptor type A.

J Nat Prod 63: 694-7 (2000)

Griffith University

2D 3D TSV

10843231

Carbonic anhydrase inhibitors: synthesis of N-morpholylthiocarbonylsulfenylamino aromatic/heterocyclic sulfonamides and their interaction with isozymes I, II and IV.

Bioorg Med Chem Lett 10: 1117-20 (2000)

Universit£ degli Studi

2D 3D TSV

129

10843230

Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity.

Bioorg Med Chem Lett 10: 1113-5 (2000)

Yale University

2D 3D TSV

10843229

Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists.

Bioorg Med Chem Lett 10: 1109-11 (2000)

R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10843226

First pharmacophoric hypothesis for 5-HT7 antagonism.

Bioorg Med Chem Lett 10: 1097-100 (2000)

Universidad Complutense

2D 3D TSV

10843225

Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.

Bioorg Med Chem Lett 10: 1093-6 (2000)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10843224

High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor.

Bioorg Med Chem Lett 10: 1089-92 (2000)

Università di Catania

2D 3D TSV

10843222

Novel alpha-glucosidase inhibitors with a tetrachlorophthalimide skeleton.

Bioorg Med Chem Lett 10: 1081-4 (2000)

University of Tokyo

2D 3D TSV

10843221

Examination of N-hydroxylation as a prerequisite mechanism of nitric oxide synthase inactivation.

Bioorg Med Chem Lett 10: 1077-80 (2000)

University at Buffalo

2D 3D TSV

10843219

Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.

Bioorg Med Chem Lett 10: 1069-72 (2000)

Merck Research Laboratories

2D 3D TSV

10843217

Synthesis and structure-activity relationship of novel pyridyl ethers for the nicotinic acetylcholine receptor.

Bioorg Med Chem Lett 10: 1063-6 (2000)

R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10843211

Structure-activity relationship studies of flavopiridol analogues.

Bioorg Med Chem Lett 10: 1037-41 (2000)

Mitotix Inc

2D 3D TSV

10843204

Synthesis of glycolipid analogues that disrupt binding of HIV-1 gp120 to galactosylceramide.

Bioorg Med Chem Lett 10: 1011-4 (2000)

Cornell University

2D 3D TSV

10843203

Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands.

Bioorg Med Chem Lett 10: 1007-10 (2000)

Glaxo Wellcome

2D 3D TSV

10841807

Modeling cyclooxygenase inhibition. Implication of active site hydration on the selectivity of ketoprofen analogues.

J Med Chem 43: 2280-4 (2000)

Laboratorios Menarini

2D 3D TSV

10841803

Anilides of (R)-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase.

J Med Chem 43: 2248-57 (2000)

Novartis Institute for Biomedical Research

2D 3D TSV

10841802

Novel inhibitors of nucleoside triphosphate diphosphohydrolases: chemical synthesis and biochemical and pharmacological characterizations.

J Med Chem 43: 2239-47 (2000)

Universit£ de Sherbrooke

2D 3D TSV

10841801

Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.

J Med Chem 43: 2227-38 (2000)

Vrije Universiteit

2D 3D TSV

10841800

Novel potent ligands for the central nicotinic acetylcholine receptor: synthesis, receptor binding, and 3D-QSAR analysis.

J Med Chem 43: 2217-26 (2000)

NeuroSearch A/S

2D 3D TSV

10841798

Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.

J Med Chem 43: 2196-203 (2000)

National Institute of Diabetes

2D 3D TSV

10841797

Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.

J Med Chem 43: 2183-95 (2000)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

110

10841794

Structure-activity relationships in a series of bisquaternary bisphthalimidine derivatives modulating the muscarinic M(2)-receptor allosterically.

J Med Chem 43: 2155-64 (2000)

University of W�rzburg

2D 3D TSV

10841791

Modeling of kappa-opioid receptor/agonists interactions using pharmacophore-based and docking simulations.

J Med Chem 43: 2124-34 (2000)

Universit£ di Napoli"Federico II"

2D 3D TSV

10841790

Synthesis, molecular modeling, and opioid receptor affinity of 9, 10-diazatricyclo[4.2.1.1(2,5)]decanes and 2,7-diazatricyclo[4.4.0. 0(3,8)]decanes structurally related to 3,8-diazabicyclo[3.2. 1]octanes.

J Med Chem 43: 2115-23 (2000)

Istituto di Chimica Farmaceutica e Tossicologica

2D 3D TSV

10841789

Developing a dynamic pharmacophore model for HIV-1 integrase.

J Med Chem 43: 2100-14 (2000)

University of California

2D 3D TSV

10840050

Multidrug-resistance protein 5 is a multispecific organic anion transporter able to transport nucleotide analogs.

Proc Natl Acad Sci U S A 97: 7476-81 (2000)

The Netherlands Cancer Institute

2D 3D TSV

10832613

[3H]S33084: a novel, selective and potent radioligand at cloned, human dopamine D3 receptors.

Naunyn Schmiedebergs Arch Pharmacol 361: 569-72 (2000)

Croissy-sur-Seine Paris

2D 3D TSV

10825466

Role of organic cation transporters in the renal secretion of nucleosides.

Biochem Pharmacol 60: 215-9 (2000)

The University of Texas M.D. Anderson Cancer Center

2D 3D TSV

10825452

Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta.

Biochim Biophys Acta 1466: 315-27 (2000)

Medical College of Georgia

2D 3D TSV

10821800

Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors.

Br J Pharmacol 130: 692-8 (2000)

Friedrich-Schiller-University Jena

2D 3D TSV

10821720

7-Methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine: a new heterocyclic system and a new lead compound for dopamine receptor antagonists.

J Med Chem 43: 2079-81 (2000)

University of Bonn

2D 3D TSV

10821718

Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter.

J Med Chem 43: 2064-71 (2000)

Georgetown University Medical Center

2D 3D TSV

10821717

Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety.

J Med Chem 43: 2049-63 (2000)

Takeda Chemical Industries, Ltd

2D 3D TSV

10821716

Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.

J Med Chem 43: 2040-8 (2000)

Shionogi & Co., Ltd.

2D 3D TSV

10821715

A new class of HIV-1 integrase inhibitors: the 3,3,3', 3'-tetramethyl-1,1'-spirobi(indan)-5,5',6,6'-tetrol family.

J Med Chem 43: 2031-9 (2000)

University of California

2D 3D TSV

10821714

Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.

J Med Chem 43: 2019-30 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10821713

SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues.

J Med Chem 43: 2007-18 (2000)

University of Bologna

2D 3D TSV

10821712

Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity.

J Med Chem 43: 1993-2006 (2000)

NeoGenesis, Inc.

2D 3D TSV

10821708

4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.

J Med Chem 43: 1958-68 (2000)

Eli Lilly and Company

2D 3D TSV

138

10821707

Modeling of the inhibition of retroviral integrases by styrylquinoline derivatives.

J Med Chem 43: 1949-57 (2000)

CNRS UMR 8532

2D 3D TSV

10821705

Synthesis and evaluation of"AZT-HEPT","AZT-pyridinone", and"ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase.

J Med Chem 43: 1927-39 (2000)

Institut Curie

2D 3D TSV

10821704

Design and synthesis of Cyclopenta[g]quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents(,).

J Med Chem 43: 1910-26 (2000)

The Institute of Cancer Research

2D 3D TSV

10821703

Application of similarity matrices and genetic neural networks in quantitative structure-activity relationships of 2- or 4-(4-Methylpiperazino)pyrimidines: 5-HT(2A) receptor antagonists.

J Med Chem 43: 1901-9 (2000)

Jagiellonian University

2D 3D TSV

10820137

Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.

Drug Metab Dispos 28: 655-60 (2000)

Vanderbilt University School of Medicine

2D 3D TSV

10818260

Selective somatostatin sst(2) receptor blockade with the novel cyclic octapeptide, CYN-154806.

Neuropharmacology 39: 1443-50 (2000)

University of Cambridge

2D 3D TSV

10794706

Subtype-selective N-methyl-D-aspartate receptor antagonists: benzimidazalone and hydantoin as phenol replacements.

J Med Chem 43: 1892-7 (2000)

CoCensys Inc

2D 3D TSV

10794705

Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.

J Med Chem 43: 1886-91 (2000)

Sapienza University of Rome

2D 3D TSV

10794704

Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat.

J Med Chem 43: 1878-85 (2000)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10794702

Protease inhibitors: synthesis of potent bacterial collagenase and matrix metalloproteinase inhibitors incorporating N-4-nitrobenzylsulfonylglycine hydroxamate moieties.

J Med Chem 43: 1858-65 (2000)

Università degli Studi

2D 3D TSV

340

10794701

Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol.

J Med Chem 43: 1852-7 (2000)

University of Bristol

2D 3D TSV

10794700

1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.

J Med Chem 43: 1841-51 (2000)

Universitat des Saarlandes

2D 3D TSV

10794697

Multivariate data analysis using D-optimal designs, partial least squares, and response surface modeling: A directional approach for the analysis of farnesyltransferase inhibitors.

J Med Chem 43: 1807-16 (2000)

Rhône-Poulenc Rorer

2D 3D TSV

10794696

Protease inhibitors: synthesis and QSAR study of novel classes of nonbasic thrombin inhibitors incorporating sulfonylguanidine and O-methylsulfonylisourea moieties at P1.

J Med Chem 43: 1793-806 (2000)

Universit£ degli Studi

2D 3D TSV

233

10794694

Design of a Gag pentapeptide analogue that binds human cyclophilin A more efficiently than the entire capsid protein: new insights for the development of novel anti-HIV-1 drugs.

J Med Chem 43: 1770-9 (2000)

Departement D'Ingenierie et D'Etudes des Proteines

2D 3D TSV

10794692

Characterization of the binding site of the histamine H(3) receptor. 2. Synthesis, in vitro pharmacology, and QSAR of a series of monosubstituted benzyl analogues of thioperamide.

J Med Chem 43: 1754-61 (2000)

Vrije Universiteit

2D 3D TSV

10794691

Solution structures in SDS micelles and functional activity at the bullfrog substance P receptor of ranatachykinin peptides.

J Med Chem 43: 1741-53 (2000)

Marshall University School of Medicine and Huntington VA Medical Center

2D 3D TSV

10794689

Design and synthesis of conformationally constrained glucagon analogues.

J Med Chem 43: 1714-22 (2000)

University of Arizona

2D 3D TSV

10794688

New proline mimetics: synthesis of thrombin inhibitors incorporating cyclopentane- and cyclopentenedicarboxylic acid templates in the P2 position. Binding conformation investigated by X-ray crystallography.

J Med Chem 43: 1705-13 (2000)

Link£ping University

2D 3D TSV

10794687

2-amino-2-oxazolines as subtype selective alpha(2) adrenoceptor agonists.

J Med Chem 43: 1699-704 (2000)

Lundbeck Research USA, Inc.

2D 3D TSV

10794686

Probing the conformation of the sugar transport inhibitor phlorizin by 2D-NMR, molecular dynamics studies, and pharmacophore analysis.

J Med Chem 43: 1692-8 (2000)

Max-Planck-Institut f£r molekulare Physiologie

2D 3D TSV

10794685

Molecular determinants of MAO selectivity in a series of indolylmethylamine derivatives: biological activities, 3D-QSAR/CoMFA analysis, and computational simulation of ligand recognition.

J Med Chem 43: 1684-91 (2000)

Universitat Autònoma de Barcelona

2D 3D TSV

10794684

Substituted benzamide inhibitors of human rhinovirus 3C protease: structure-based design, synthesis, and biological evaluation.

J Med Chem 43: 1670-83 (2000)

Agouron Pharmaceuticals Inc

2D 3D TSV

10794683

Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration.

J Med Chem 43: 1664-9 (2000)

Novo Nordisk A/S

2D 3D TSV

10794682

N-[[(5-methyl-3-phenylisoxazol-4-yl)-phenyl]sulfonyl]propanamide, sodium salt, parecoxib sodium: A potent and selective inhibitor of COX-2 for parenteral administration.

J Med Chem 43: 1661-3 (2000)

Pfizer Inc

2D 3D TSV

10794681

Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents.

J Med Chem 43: 1641-60 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10785418

Halogenated boldine derivatives with enhanced monoamine receptor selectivity.

J Nat Prod 63: 480-4 (2000)

Universidad de Chile

2D 3D TSV

10785413

Bioactive compounds from Combretum erythrophyllum.

J Nat Prod 63: 457-60 (2000)

Virginia Polytechnic Institute and State University

2D 3D TSV

10782696

ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.

Bioorg Med Chem Lett 10: 831-4 (2000)

F. Hoffmann-La Roche Inc

2D 3D TSV

10782692

Leukotriene B4 photoaffinity probes: design, synthesis and evaluation of new arylazide-1,3-disubstituted cyclohexanes.

Bioorg Med Chem Lett 10: 811-4 (2000)

UPRESA-CNRS 5074

2D 3D TSV

10782691

Novel 3-(4-piperidinylthio)-1H-indoles as potent nonopioid orally active central analgesics.

Bioorg Med Chem Lett 10: 805-9 (2000)

Laboratoires UPSA

2D 3D TSV

10782686

The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.

Bioorg Med Chem Lett 10: 783-6 (2000)

Wyeth-Ayerst Research

2D 3D TSV

10782685

Synthesis of a cyanopeptide-analogue with trypsin activating properties.

Bioorg Med Chem Lett 10: 779-81 (2000)

Ernst-Moritz-Arndt-University

2D 3D TSV

10782682

QSAR of 1,1'-(1,2-ethylenebisbenzyl)bis(4-substitutedpyridinium) dibromides as choline kinase inhibitors: a different approach for antiproliferative drug design.

Bioorg Med Chem Lett 10: 767-70 (2000)

Granada

2D 3D TSV

10782677

Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.

Bioorg Med Chem Lett 10: 745-9 (2000)

Corvas International Inc

2D 3D TSV

10782674

N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.

Bioorg Med Chem Lett 10: 729-33 (2000)

Hoffmann-La Roche Inc

2D 3D TSV

10782673

N-acyl phenylalanine analogues as potent small molecule VLA-4 antagonists.

Bioorg Med Chem Lett 10: 725-7 (2000)

Roche Research Center

2D 3D TSV

10782670

Alpha-ketoamides, alpha-ketoesters and alpha-diketones as HCV NS3 protease inhibitors.

Bioorg Med Chem Lett 10: 711-3 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10782669

Synthesis and biological activity of fluoro-substituted pyrrolo[2,3-d]pyrimidines: the development of potential positron emission tomography imaging agents for the corticotropin-releasing hormone type 1 receptor.

Bioorg Med Chem Lett 10: 707-10 (2000)

NIDDK

2D 3D TSV

10782666

The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.

Bioorg Med Chem Lett 10: 695-8 (2000)

Wyeth-Ayerst Research

2D 3D TSV

10782664

Isoxazolines and isoxazoles as factor Xa inhibitors.

Bioorg Med Chem Lett 10: 685-9 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10780918

Syntheses of (R)- and (S)-2- and 6-fluoronorepinephrine and (R)- and (S)-2- and 6-fluoroepinephrine: effect of stereochemistry on fluorine-induced adrenergic selectivities.

J Med Chem 43: 1611-9 (2000)

National Institute of Diabetes and Digestive and Kidney Diseases

2D 3D TSV

10780916

Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).

J Med Chem 43: 1586-603 (2000)

Abbott Laboratories

2D 3D TSV

134

10780914

Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists.

J Med Chem 43: 1573-6 (2000)

University of Minnesota

2D 3D TSV

10780912

Structural studies on bioactive compounds. 32. Oxidation of tyrphostin protein tyrosine kinase inhibitors with hypervalent iodine reagents.

J Med Chem 43: 1550-62 (2000)

University of Nottingham

2D 3D TSV

10780910

Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture.

J Med Chem 43: 1533-40 (2000)

Université Paris-Sud

2D 3D TSV

10780908

AMP deaminase inhibitors. 4. Further N3-substituted coformycin aglycon analogues: N3-alkylmalonates as ribose 5'-monophosphate mimetics.

J Med Chem 43: 1519-24 (2000)

Metabasis Therapeutics Inc

2D 3D TSV

10780907

AMP deaminase inhibitors. 3. SAR of 3-(carboxyarylalkyl)coformycin aglycon analogues.

J Med Chem 43: 1508-18 (2000)

Metabasis Therapeutics Inc

2D 3D TSV

10780906

AMP deaminase inhibitors. 2. Initial discovery of a non-nucleotide transition-state inhibitor series.

J Med Chem 43: 1495-507 (2000)

Metabasis Therapeutics Inc

2D 3D TSV

10780903

Study on selectin blocker. 8. Lead discovery of a non-sugar antagonist using a 3D-pharmacophore model.

J Med Chem 43: 1476-83 (2000)

Nippon Organon K.K.

2D 3D TSV

10780900

A study of the relationship between biological activity and prolyl amide isomer geometry in oxytocin using 5-tert-butylproline to augment the Cys(6)-Pro(7) amide cis-isomer population.

J Med Chem 43: 1448-55 (2000)

Université de Montréal

2D 3D TSV

10780899

GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology.

J Med Chem 43: 1427-47 (2000)

University of Sydney

2D 3D TSV

10779411

Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.

Chem Biol 7: 299-312 (2000)

Axys Pharmaceutical

2D 3D TSV

10779381

[(3)H]MRE 3008F20: a novel antagonist radioligand for the pharmacological and biochemical characterization of human A(3) adenosine receptors.

Mol Pharmacol 57: 968-75 (2000)

University of Ferrara

2D 3D TSV

10777579

Thermodynamic consequences of grafting enhanced affinity toward the mutated antigen onto an antibody. The case of anti-lysozyme antibody, HyHEL-10.

J Biol Chem 275: 12813-20 (2000)

Tohoku University

2D 3D TSV

10777500

Distinct Ca2+ binding properties of novel C2 domains of plant phospholipase dalpha and beta.

J Biol Chem 275: 19700-6 (2000)

Kansas State University

2D 3D TSV

10773045

Characterization of a tropane radioligand, [(3)H]2beta-propanoyl-3beta-(4-tolyl) tropane ([(3)H]PTT), for dopamine transport sites in rat brain.

J Pharmacol Exp Ther 293: 686-96 (2000)

Wake Forest University

2D 3D TSV

10773005

Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein.

J Pharmacol Exp Ther 293: 376-82 (2000)

Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology

2D 3D TSV

10762053

Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor.

Bioorg Med Chem Lett 10: 681-4 (2000)

Università di Ferrara

2D 3D TSV

10762051

Carbonic anhydrase inhibitors: topical sulfonamide antiglaucoma agents incorporating secondary amine moieties.

Bioorg Med Chem Lett 10: 673-6 (2000)

Universit£ degli Studi

2D 3D TSV

10762050

Inhibition of the ras-dependent mitogenic pathway by phosphopeptide prodrugs with antiproliferative properties.

Bioorg Med Chem Lett 10: 669-72 (2000)

University of Paris

2D 3D TSV

10762046

Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effect of constraining the glycerol backbone in DAG lactones.

Bioorg Med Chem Lett 10: 653-5 (2000)

National Cancer Institute-Bethesda

2D 3D TSV

10762045

The solid phase synthesis of tetrahydroisoquinolines having cdc25B inhibitory activity.

Bioorg Med Chem Lett 10: 649-52 (2000)

Pharmacia & Upjohn

2D 3D TSV

10762042

Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts.

Bioorg Med Chem Lett 10: 637-9 (2000)

CNRS

2D 3D TSV

10762041

Parallel synthesis of a library of 1,4-naphthoquinones and automated screening of potential inhibitors of trypanothione reductase from Trypanosoma cruzi.

Bioorg Med Chem Lett 10: 631-5 (2000)

Université Lille II

2D 3D TSV

10762040

Yohimbine dimers exhibiting binding selectivities for human alpha2a- versus alpha2b-adrenergic receptors.

Bioorg Med Chem Lett 10: 627-30 (2000)

University of Tennessee

2D 3D TSV

10762039

Syntheses and evaluation of naphthalenyl- and chromenyl-pyrrolyl-benzoic acids as potent and selective retinoic acid receptor alpha agonists.

Bioorg Med Chem Lett 10: 623-5 (2000)

Eisai Co., Ltd

2D 3D TSV

10762038

Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives.

Bioorg Med Chem Lett 10: 619-22 (2000)

Eisai Co., Ltd

2D 3D TSV

10762037

Synthesis of a novel class of cdc25A inhibitors from vitamin D3.

Bioorg Med Chem Lett 10: 615-7 (2000)

The University of Tokyo

2D 3D TSV

10760098

ATP-dependent para-aminohippurate transport by apical multidrug resistance protein MRP2.

Kidney Int 57: 1636-42 (2000)

Deutsches Krebsforschungszentrum

2D 3D TSV

10757731

Two new prenylated 3-benzoxepin derivatives as cyclooxygenase inhibitors from Perilla frutescens var. acuta.

J Nat Prod 63: 403-5 (2000)

Columbia University

2D 3D TSV

10757728

Isolation of psammaplin A 11'-sulfate and bisaprasin 11'-sulfate from the marine sponge Aplysinella rhax.

J Nat Prod 63: 393-5 (2000)

Griffith University

2D 3D TSV

10757727

Three new triterpenoids from Peganum nigellastrum.

J Nat Prod 63: 390-2 (2000)

Toho University

2D 3D TSV

10757710

Anthoptilides A-E, new Briarane diterpenes from the Australian sea pen Anthoptilum cf. kukenthali.

J Nat Prod 63: 318-21 (2000)

Griffith University

2D 3D TSV

10757709

Luteolin, a compound with adenosine A(1) receptor-binding activity, and chromone and dihydronaphthalenone constituents from Senna siamea.

J Nat Prod 63: 315-7 (2000)

Leiden University

2D 3D TSV

10755640

18F-labeled FECNT: a selective radioligand for PET imaging of brain dopamine transporters.

Nucl Med Biol 27: 1-12 (2000)

Emory University

2D 3D TSV

10754449

In vitro pharmacological profile of SK-896, a new human motilin analogue.

Pharmacology 60: 128-35 (2000)

Sanwa Kagaku Kenkyusho Co., Ltd

2D 3D TSV

10753480

Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.

J Med Chem 43: 1423-6 (2001)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10753478

Inhibition of protein kinase C(alpha) by dequalinium analogues: dependence on linker length and geometry.

J Med Chem 43: 1413-7 (2000)

The City University of New York

2D 3D TSV

10753476

Phosphinic derivatives as new dual enkephalin-degrading enzyme inhibitors: synthesis, biological properties, and antinociceptive activities.

J Med Chem 43: 1398-408 (2001)

University of Paris

2D 3D TSV

10753475

Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.

J Med Chem 43: 1380-97 (2001)

University of Auckland

2D 3D TSV

10753473

Deltorphin II analogues with 6-hydroxy-2-aminotetralin-2-carboxylic acid in position 1.

J Med Chem 43: 1359-66 (2001)

Hungarian Academy of Sciences

2D 3D TSV

10753471

Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.

J Med Chem 43: 1339-49 (2001)

Uppsala University

2D 3D TSV

10753470

High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.

J Med Chem 43: 1329-38 (2001)

F. Hoffmann-La Roche Inc

2D 3D TSV

10753467

Novel benzofuran and benzothiophene biphenyls as inhibitors of protein tyrosine phosphatase 1B with antihyperglycemic properties.

J Med Chem 43: 1293-310 (2001)

Wyeth-Ayerst Research

2D 3D TSV

118

10753466

Cyclin-dependent kinase inhibition by new C-2 alkynylated purine derivatives and molecular structure of a CDK2-inhibitor complex.

J Med Chem 43: 1282-92 (2000)

Institut Curie

2D 3D TSV

10753465

Conformational selection of inhibitors and substrates by proteolytic enzymes: implications for drug design and polypeptide processing.

J Med Chem 43: 1271-81 (2001)

University of Queensland

2D 3D TSV

10753463

N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.

J Med Chem 43: 1257-63 (2001)

Bristol-Myers Squibb Pharmaceutical Research Institute

2D 3D TSV

10753461

Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.

J Med Chem 43: 1251-2 (2001)

University of Minnesota

2D 3D TSV

10748266

Inhibitory effect of novel oral hypoglycemic agent nateglinide (AY4166) on peptide transporters PEPT1 and PEPT2.

Eur J Pharmacol 392: 11-7 (2000)

Kyoto University Hospital

2D 3D TSV

10747922

Compulsory order of substrate binding to herpes simplex virus type 1 thymidine kinase. A calorimetric study.

J Biol Chem 275: 16139-45 (2000)

Swiss Federal Institute of Technology

2D 3D TSV

10746010

Solid-phase synthesis of a combinatorial array of 1,3-bis(acylamino)-2-butanones, inhibitors of the cysteine proteases cathepsins K and L.

J Comb Chem 1: 207-15 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10743959

N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists.

Bioorg Med Chem Lett 10: 509-12 (2000)

Yoshitomi Pharmaceutical Industries Ltd

2D 3D TSV

10743958

Solid phase synthesis of diamides as potential bone resorption inhibitors.

Bioorg Med Chem Lett 10: 503-7 (2000)

AstraZeneca R & D M£lndal

2D 3D TSV

10743957

Protease inhibitors: synthesis of clostridium histolyticum collagenase inhibitors incorporating sulfonyl-L-alanine hydroxamate moieties.

Bioorg Med Chem Lett 10: 499-502 (2000)

Università degli Studi

2D 3D TSV

10743955

Selection of a potent inhibitor of trihydroxynaphthalene reductase by sorting disease control data.

Bioorg Med Chem Lett 10: 491-4 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10743953

The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: hydroxyindole derivatives.

Bioorg Med Chem Lett 10: 483-6 (2000)

State University of New York

2D 3D TSV

10743952

The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 1: hydroxynaphthalene derivatives.

Bioorg Med Chem Lett 10: 477-81 (2000)

State University of New York

2D 3D TSV

10743951

Synthesis of enantiomerically pure (+)- and (-)-18-methoxycoronaridine hydrochloride and their preliminary assessment as anti-addictive agents.

Bioorg Med Chem Lett 10: 473-6 (2000)

Albany Molecular Research, Inc.

2D 3D TSV

10743949

(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.

Bioorg Med Chem Lett 10: 465-8 (2000)

Università di Perugia

2D 3D TSV

10743948

5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.

Bioorg Med Chem Lett 10: 461-4 (2000)

Ewha Womans University

2D 3D TSV

10743947

Synthesis and characterization of a novel class of protein tyrosine phosphatase inhibitors.

Bioorg Med Chem Lett 10: 457-60 (2000)

New York University

2D 3D TSV

10743946

Synthesis of neurotensin(9-13) analogues exhibiting enhanced human neurotensin receptor binding affinities.

Bioorg Med Chem Lett 10: 453-5 (2000)

Medical University of South Carolina

2D 3D TSV

10743945

Ring constrained analogues of beta-alanine-containing GPIIb/IIIa receptor antagonists.

Bioorg Med Chem Lett 10: 449-52 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10743944

Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides.

Bioorg Med Chem Lett 10: 443-7 (2000)

Merck Research Laboratories

2D 3D TSV

10743942

Design and synthesis of mimics of S-adenosyl-L-homocysteine as potential inhibitors of erythromycin methyltransferases.

Bioorg Med Chem Lett 10: 433-7 (2000)

Université de Montréal

2D 3D TSV

10743939

Synthesis and biological activities of NB-506 analogues modified at the glucose group.

Bioorg Med Chem Lett 10: 419-22 (2000)

Banyu Tsukuba Research Institute

2D 3D TSV

10743938

Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.

Bioorg Med Chem Lett 10: 415-8 (2000)

Ligand Pharmaceuticals

2D 3D TSV

103

10743937

Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines.

Bioorg Med Chem Lett 10: 411-4 (2000)

Ligand Pharmaceuticals

2D 3D TSV

10743936

Irreversible inhibition of type I dehydroquinase by substrates for type II dehydroquinase.

Bioorg Med Chem Lett 10: 407-9 (2000)

University Chemical Laboratory

2D 3D TSV

10741563

Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand.

Bioorg Med Chem Lett 10: 605-7 (2000)

University of Bristol

2D 3D TSV

10741562

1,3-Diarylcycloalkanopyrazoles and diphenyl hydrazides as selective inhibitors of cyclooxygenase-2.

Bioorg Med Chem Lett 10: 601-4 (2000)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10741561

Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine.

Bioorg Med Chem Lett 10: 597-600 (2000)

Glaxo Wellcome Research and Development

2D 3D TSV

10741557

Naphthyl ketones: a new class of Janus kinase 3 inhibitors.

Bioorg Med Chem Lett 10: 575-9 (2000)

AstraZeneca

2D 3D TSV

10741555

2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity.

Bioorg Med Chem Lett 10: 567-9 (2000)

Universität Hamburg

2D 3D TSV

10741553

Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.

Bioorg Med Chem Lett 10: 559-62 (2000)

Bristol-Myers Squibb Pharmaceutical Research Institute

2D 3D TSV

10741546

Parallel synthesis of a series of subtype-selective NMDA receptor antagonists.

Bioorg Med Chem Lett 10: 527-9 (2000)

Parke-Davis Pharmaceutical Research

2D 3D TSV

10741545

Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.

Bioorg Med Chem Lett 10: 523-6 (2000)

Pfizer Inc

2D 3D TSV

10737756

Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.

J Med Chem 43: 1234-41 (2000)

Merck Research Laboratories

2D 3D TSV

10737755

Novel and selective calcitonin-inducing agents.

J Med Chem 43: 1223-33 (2000)

Wyeth-Ayerst Research

2D 3D TSV

10737754

Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors.

J Med Chem 43: 1215-22 (2000)

Georgetown University Medical Center

2D 3D TSV

10737750

SH2-directed ligands of the Lck tyrosine kinase.

J Med Chem 43: 1173-9 (2000)

The Albert Einstein College of Medicine

2D 3D TSV

10737749

Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.

J Med Chem 43: 1165-72 (2000)

National Institute of Diabetes

2D 3D TSV

182

10737748

1,2,4-Triazolo[4,3-a]quinoxalin-1-one: a versatile tool for the synthesis of potent and selective adenosine receptor antagonists.

J Med Chem 43: 1158-64 (2000)

Universita' di Firenze

2D 3D TSV

10737747

5-HT reuptake inhibitors with 5-HT(1B/1D) antagonistic activity: a new approach toward efficient antidepressants.

J Med Chem 43: 1149-57 (2000)

Merck KGaA

2D 3D TSV

10737745

Investigating protein-ligand interactions with a mutant FKBP possessing a designed specificity pocket.

J Med Chem 43: 1135-42 (2000)

ARIAD Gene Therapeutics, Inc.

2D 3D TSV

10737744

Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.

J Med Chem 43: 1123-34 (2000)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

146

10737743

3D-QSAR CoMFA study on imidazolinergic I(2) ligands: a significant model through a combined exploration of structural diversity and methodology.

J Med Chem 43: 1109-22 (2000)

Universit£ d'Orl£ans

2D 3D TSV

119

10737742

2',6'-Dimethylphenoxyacetyl: a new achiral high affinity P(3)-P(2) ligand for peptidomimetic-based HIV protease inhibitors.

J Med Chem 43: 1094-108 (2000)

Boehringer Ingelheim Pharmaceuticals Inc

2D 3D TSV

10737741

Highly selective chiral N-substituted 3alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues for the dopamine transporter: synthesis and comparative molecular field analysis.

J Med Chem 43: 1085-93 (2000)

National Institute on Drug Abuse-Intramural Research Program

2D 3D TSV

10737740

Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.

J Med Chem 43: 1071-84 (2000)

Freie Universit£t Berlin

2D 3D TSV

10737739

Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants.

J Med Chem 43: 1062-70 (2000)

National Eye Institute

2D 3D TSV

10737738

Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles.

J Med Chem 43: 1050-61 (2000)

King's College London

2D 3D TSV

10737736

Pyrrolidine inhibitors of human cytosolic phospholipase A(2).

J Med Chem 43: 1041-4 (2000)

Shionogi & Company, Ltd.

2D 3D TSV

10732980

Protease inhibitors. Part 8: synthesis of potent Clostridium histolyticum collagenase inhibitors incorporating sulfonylated L-alanine hydroxamate moieties.

Bioorg Med Chem 8: 637-45 (2000)

Universita degli Studi di Firenze

2D 3D TSV

10732965

Acetylcholinesterase inhibitors for potential use in Alzheimer's disease: molecular modeling, synthesis and kinetic evaluation of 11H-indeno-[1,2-b]-quinolin-10-ylamine derivatives.

Bioorg Med Chem 8: 497-506 (2000)

University of Bologna

2D 3D TSV

10729360

Inhibition of the P-glycoprotein- and multidrug resistance protein-mediated efflux of anthracyclines and calceinacetoxymethyl ester by PAK-104P.

Eur J Pharmacol 391: 207-16 (2000)

Universit£ Paris Nord

2D 3D TSV

10715167

Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.

J Med Chem 43: 1034-40 (2000)

Upjohn

2D 3D TSV

10715164

2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.

J Med Chem 43: 1011-8 (2000)

Virginia Commonwealth University

2D 3D TSV

10715163

New azolidinediones as inhibitors of protein tyrosine phosphatase 1B with antihyperglycemic properties.

J Med Chem 43: 995-1010 (2000)

Wyeth-Ayerst Research

2D 3D TSV

10715162

Synthesis of N-substituted 4-(4-hydroxyphenyl)piperidines, 4-(4-hydroxybenzyl)piperidines, and (+/-)-3-(4-hydroxyphenyl)pyrrolidines: selective antagonists at the 1A/2B NMDA receptor subtype.

J Med Chem 43: 984-94 (2000)

CoCensys Inc

2D 3D TSV

10715159

Design and synthesis of 13,14-dihydro prostaglandin F(1alpha) analogues as potent and selective ligands for the human FP receptor.

J Med Chem 43: 945-52 (2000)

Procter and Gamble Pharmaceuticals

2D 3D TSV

112

10715158

Conformationally constrained analogues of diacylglycerol (DAG). 16. How much structural complexity is necessary for recognition and high binding affinity to protein kinase C?

J Med Chem 43: 921-44 (2000)

National Cancer Institute-Bethesda

2D 3D TSV

10715157

Inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands. 2. 4-(2-Malonyl)phenylalanine as a potent phosphotyrosyl mimetic.

J Med Chem 43: 911-20 (2000)

National Cancer Institute-Bethesda

2D 3D TSV

10715156

Selective ET(A) antagonists. 5. Discovery and structure-activity relationships of phenoxyphenylacetic acid derivatives.

J Med Chem 43: 900-10 (2000)

Rhône-Poulenc Rorer

2D 3D TSV

10715152

5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease.

J Med Chem 43: 843-58 (2000)

Parke-Davis Pharmaceutical Research

2D 3D TSV

151

10715151

Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y(1) receptor ligands.

J Med Chem 43: 829-42 (2000)

National Institute of Diabetes

2D 3D TSV

10715150

Consensus bioactive conformation of cyclic GnRH antagonists defined by NMR and molecular modeling.

J Med Chem 43: 819-28 (2000)

Salk Institute

2D 3D TSV

10715149

Design of potent dicyclic (1-5/4-10) gonadotropin releasing hormone (GnRH) antagonists.

J Med Chem 43: 807-18 (2000)

Salk Institute

2D 3D TSV

10715148

Design of monocyclic (1-3) and dicyclic (1-3/4-10) gonadotropin releasing hormone (GnRH) antagonists.

J Med Chem 43: 797-806 (2000)

Salk Institute

2D 3D TSV

10715147

Design of potent dicyclic (4-10/5-8) gonadotropin releasing hormone (GnRH) antagonists.

J Med Chem 43: 784-96 (2000)

Salk Institute

2D 3D TSV

10715145

4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.

J Med Chem 43: 775-7 (2000)

Searle Research and Development

2D 3D TSV

10715144

Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity.

J Med Chem 43: 772-4 (2000)

Georgetown University Medical Center

2D 3D TSV

10715143

1-(2-Nitrophenyl)thiosemicarbazides: a novel class of potent, orally active non-peptide antagonist for the bradykinin B(2) receptor.

J Med Chem 43: 769-71 (2000)

Novartis Institute for Medical Sciences

2D 3D TSV

10715142

alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.

J Med Chem 43: 765-8 (2000)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10714510

The discovery and synthesis of highly potent, A2a receptor agonists.

Bioorg Med Chem Lett 10: 403-6 (2000)

GlaxoWellcome Medicines Research Centre

2D 3D TSV

10714509

Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd] indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor.

Bioorg Med Chem Lett 10: 399-402 (2000)

Novo Nordisk A/S

2D 3D TSV

10714508

2-(Alkylthio)pyrimidin-4-ones as novel, reversible inhibitors of lipoprotein-associated phospholipase A2.

Bioorg Med Chem Lett 10: 395-8 (2000)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10714507

Mechanism-based inactivation of thymidylate synthase by 5-(3-fluoropropyn-1-yl)-2'-deoxyuridine 5'-phosphate.

Bioorg Med Chem Lett 10: 391-4 (2000)

State University of New York

2D 3D TSV

10714506

Fused bicyclic Gly-Asp beta-turn mimics with potent affinity for GPIIb-IIIa. Exploration of the arginine isostere.

Bioorg Med Chem Lett 10: 385-9 (2000)

Eli Lilly and Company

2D 3D TSV

10714503

Novel oximes having 5-benzyl-2,4-thiazolidinedione as antihyperglycemic agents: synthesis and structure-activity relationship.

Bioorg Med Chem Lett 10: 373-5 (2000)

Sankyo Co., Ltd

2D 3D TSV

10714498

Synthesis of 8-chloro-benzo[c]quinolizin-3-ones as potent and selective inhibitors of human steroid 5alpha-reductase 1.

Bioorg Med Chem Lett 10: 353-6 (2000)

Università di Firenze

2D 3D TSV

10714496

Design and biological evaluation of non-peptide analogues of omega-conotoxin MVIIA.

Bioorg Med Chem Lett 10: 345-7 (2000)

Parke-Davis Neuroscience Research Centre

2D 3D TSV

10714492

2-Methyladenosine-Substituted 2',5'-oligoadenylates: conformations, 2-5A binding and catalytic activities with human ribonuclease L.

Bioorg Med Chem Lett 10: 329-31 (2000)

Gifu University

2D 3D TSV

10708730

Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological medium.

Eur J Pharmacol 390: 245-8 (2000)

Eli Lilly and Company

2D 3D TSV

10698459

The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.

Bioorg Med Chem Lett 10: 301-4 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10698458

Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine.

Bioorg Med Chem Lett 10: 297-300 (2000)

Georgetown University Medical Center

2D 3D TSV

10698455

Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2.

Bioorg Med Chem Lett 10: 285-8 (2000)

Univ. de Valencia

2D 3D TSV

10698454

Probing the extended binding determinants of oligosaccharyl transferase with synthetic inhibitors of asparagine-linked glycosylation.

Bioorg Med Chem Lett 10: 281-4 (2000)

Institute of Technology

2D 3D TSV

10698453

A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 2,3-disubstituted-4-phenylquinolines.

Bioorg Med Chem Lett 10: 277-9 (2000)

Searle Discovery

2D 3D TSV

10698452

3-Imidazolylmethylaminophenylsulfonyltetrahydroquinolines, a novel series of farnesyltransferase inhibitors.

Bioorg Med Chem Lett 10: 273-5 (2000)

Bristol-Myers Squibb Pharmaceutical Research Institute

2D 3D TSV

10698450

Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation.

Bioorg Med Chem Lett 10: 265-8 (2000)

Medivir AB

2D 3D TSV

10698448

N-formyl hydroxylamine containing dipeptides: generation of a new class of vasopeptidase inhibitors.

Bioorg Med Chem Lett 10: 257-60 (2000)

Bristol-Myers Squibb Pharmaceutical Research Institute

2D 3D TSV

10698447

1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs.

Bioorg Med Chem Lett 10: 253-6 (2000)

Sapienza University of Rome

2D 3D TSV

10698445

Exploring the chiral space within the active site of alpha-thrombin with a constrained mimic of D-Phe-Pro-Arg--design, synthesis, inhibitory activity, and X-ray structure of an enzyme-inhibitor complex.

Bioorg Med Chem Lett 10: 243-7 (2000)

Universit£ de Montr£al

2D 3D TSV

10698443

Chemical and enzymatic modifications of integric acid and HIV-1 integrase inhibitory activity.

Bioorg Med Chem Lett 10: 235-8 (2000)

Merck Research Laboratories

2D 3D TSV

10698440

The discovery of potent cRaf1 kinase inhibitors.

Bioorg Med Chem Lett 10: 223-6 (2000)

Glaxo Wellcome

2D 3D TSV

10698439

Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.

Bioorg Med Chem Lett 10: 217-21 (2000)

Rhone-Poulenc Rorer

2D 3D TSV

10698438

N-(sulfonamido)alkyl[tetrahydro-1H-benzo[e]indol-2-yl]amines: potent antagonists of human neuropeptide Y Y5 receptor.

Bioorg Med Chem Lett 10: 213-6 (2000)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10698437

Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors.

Bioorg Med Chem Lett 10: 209-11 (2000)

Università di Ferrara

2D 3D TSV

10698436

Preparation of 5-(2,6-dideoxy-2-fluoro-alpha-L-talopyranosyloxy)-6-hydroxynap htho[2,3- f]quinoline-7,12-dione (FT-Alz), a new-type, potentially antitumor substance with various biological activities.

Bioorg Med Chem Lett 10: 203-7 (2000)

Institute of Bioorganic Chemistry

2D 3D TSV

10698435

Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.

Bioorg Med Chem Lett 10: 199-201 (2000)

Kyoto Pharmaceutical University

2D 3D TSV

150

10694412

Thermodynamics of substrate binding to the chaperone SecB.

Biochemistry 39: 2420-7 (2000)

Indian Institute of Science

2D 3D TSV

10692507

5-Iodo-A-85380, an alpha4beta2 subtype-selective ligand for nicotinic acetylcholine receptors.

Mol Pharmacol 57: 642-9 (2000)

National Institute on Drug Abuse

2D 3D TSV

10691729

Dolastatin 3 and two novel cyclic peptides from a palauan collection of Lyngbya majuscula.

J Nat Prod 63: 279-82 (2000)

University of California at San Diego

2D 3D TSV

10691728

Cernuosides A and B, two sucrase inhibitors from Pulsatilla cernua.

J Nat Prod 63: 276-8 (2000)

China Pharmaceutical University

2D 3D TSV

10691716

Inhibitory effects on HIV-1 protease of constituents from the wood of Xanthoceras sorbifolia.

J Nat Prod 63: 238-42 (2000)

Toyama Medical and Pharmaceutical University

2D 3D TSV

10691700

Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.

J Med Chem 43: 756-62 (2000)

Friedrich-Alexander University

2D 3D TSV

112

10691697

Structure-activity relationship studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.

J Med Chem 43: 721-35 (2000)

Searle Research and Development

2D 3D TSV

133

10691696

A new class of conformationally rigid analogues of 4-amino-5-halopentanoic acids, potent inactivators of gamma-aminobutyric acid aminotransferase.

J Med Chem 43: 706-20 (2000)

Northwestern University

2D 3D TSV

10691695

Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic acids as leukotriene biosynthesis inhibitors.

J Med Chem 43: 690-705 (2000)

Abbott Laboratories

2D 3D TSV

10691694

Benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]thiadiazine 2,2-dioxides: first phosphodiesterase 7 inhibitors.

J Med Chem 43: 683-9 (2000)

Instituto de Química Médica

2D 3D TSV

10691693

Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.

J Med Chem 43: 675-82 (2000)

Novartis Pharma AG

2D 3D TSV

10691692

Inhibitors of tripeptidyl peptidase II. 2. Generation of the first novel lead inhibitor of cholecystokinin-8-inactivating peptidase: a strategy for the design of peptidase inhibitors.

J Med Chem 43: 664-74 (2000)

University College London

2D 3D TSV

10691690

Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2beta-carbo-1'-fluoro-2-propoxy-3beta-(4-chlorophenyl)tr opanes. Ligands for the imaging of dopamine transporters by positron emission tomography.

J Med Chem 43: 639-48 (2000)

Emory University

2D 3D TSV

10691686

Binding and preliminary evaluation of 5-hydroxy- and 10-hydroxy-2,3, 12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-ij]isoquinolines as dopamine receptor ligands.

J Med Chem 43: 599-608 (2000)

Universit£ di Camerino

2D 3D TSV

10691684

Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring.

J Med Chem 43: 581-90 (2000)

University of Tennessee at Memphis

2D 3D TSV

10691683

Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.

J Med Chem 43: 569-80 (2000)

University of Arizona

2D 3D TSV

10691681

Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.

J Med Chem 43: 551-9 (2000)

Clinical Research Institute of Montr£al

2D 3D TSV

10691680

The PPARs: from orphan receptors to drug discovery.

J Med Chem 43: 527-50 (2000)

Glaxo Wellcome Research & Development

2D 3D TSV

10688634

Kinetic and selectivity differences between rodent, rabbit, and human organic cation transporters (OCT1).

J Pharmacol Exp Ther 292: 1146-52 (2000)

University of California

2D 3D TSV

10688601

Cloning and pharmacological characterization of the rat CB(2) cannabinoid receptor.

J Pharmacol Exp Ther 292: 886-94 (2000)

Virginia Commonwealth University

2D 3D TSV

10681378

Interactions of HIV protease inhibitors with a human organic cation transporter in a mammalian expression system.

Drug Metab Dispos 28: 329-34 (2000)

University of California

2D 3D TSV

10673109

Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.

Bioorg Med Chem Lett 10: 193-5 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10673107

8-Aminocyclazocine analogues: synthesis and structure-activity relationships.

Bioorg Med Chem Lett 10: 183-7 (2000)

Institute

2D 3D TSV

10673106

RGD mimetics containing a central hydantoin scaffold: alpkha(v)beta3 vs alpha(IIb)beta3 selectivity requirements.

Bioorg Med Chem Lett 10: 179-82 (2000)

Hoechst Marion Roussel Inc

2D 3D TSV

10673105

Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists.

Bioorg Med Chem Lett 10: 175-8 (2000)

Synaptic Pharmaceutical Corporation

2D 3D TSV

10673103

Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists.

Bioorg Med Chem Lett 10: 167-70 (2000)

AstraZeneca R&D Montréal

2D 3D TSV

10673101

The flavanolignan silybin and its hemisynthetic derivatives, a novel series of potential modulators of P-glycoprotein.

Bioorg Med Chem Lett 10: 157-60 (2000)

Universit£ Claude Bernard Lyon 1

2D 3D TSV

10673099

Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.

Bioorg Med Chem Lett 10: 147-51 (2000)

Wyeth-Ayerst Research

2D 3D TSV

10673095

First enantiospecific synthesis of a 3,4-dihydroxy-L-glutamic acid [(3S,4S)-DHGA], a new mGluR1 agonist.

Bioorg Med Chem Lett 10: 129-33 (2000)

CNRS

2D 3D TSV

10669578

New selective and potent 5-HT(1B/1D) antagonists: chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides.

J Med Chem 43: 517-25 (2000)

University of Groningen

2D 3D TSV

10669576

Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.

J Med Chem 43: 488-504 (2000)

Novartis Institute for BioMedical Research

2D 3D TSV

10669572

4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist.

J Med Chem 43: 449-56 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10669571

Water-soluble phosphate prodrugs of 1-propargyl-8-styrylxanthine derivatives, A(2A)-selective adenosine receptor antagonists.

J Med Chem 43: 440-8 (2000)

University of Würzburg

2D 3D TSV

10669570

Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635.

J Med Chem 43: 432-9 (2000)

University of Groningen

2D 3D TSV

10669569

Synthesis, molecular modeling, and pharmacological testing of bis-quinolinium cyclophanes: potent, non-peptidic blockers of the apamin-sensitive Ca(2+)-activated K(+) channel.

J Med Chem 43: 420-31 (2000)

University College London

2D 3D TSV

10669568

Syntheses and structure-activity relationships of 5,6,7, 8-tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline derivatives with retinoic acid receptor alpha agonistic activity.

J Med Chem 43: 409-19 (2000)

Eisai Co., Ltd

2D 3D TSV

10669567

Successful virtual screening of a chemical database for farnesyltransferase inhibitor leads.

J Med Chem 43: 401-8 (2000)

Mayo Medical School and Mayo Clinic

2D 3D TSV

10669566

Derivation of pharmacophore and CoMFA models for leukotriene D(4) receptor antagonists of the quinolinyl(bridged)aryl series.

J Med Chem 43: 392-400 (2000)

Laboratorios Menarini

2D 3D TSV

10669565

Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.

J Med Chem 43: 381-91 (2000)

University of Minnesota

2D 3D TSV

10669564

Design and synthesis of piperazine-based matrix metalloproteinase inhibitors.

J Med Chem 43: 369-80 (2000)

Procter and Gamble Pharmaceuticals

2D 3D TSV

189

10669563

Structural basis of the thrombin selectivity of a ligand that contains the constrained arginine mimic (2S)-2-amino-(3S)-3-(1-carbamimidoyl- piperidin-3-yl)-propanoic acid at P1.

J Med Chem 43: 361-8 (2000)

Warner-Lambert Company

2D 3D TSV

10669562

Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies.

J Med Chem 43: 351-60 (2000)

Georgetown University Medical Center

2D 3D TSV

10669561

alpha-Substituted N-(sulfonamido)alkyl-beta-aminotetralins: potent and selective neuropeptide Y Y5 receptor antagonists.

J Med Chem 43: 346-50 (2000)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10669560

A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).

J Med Chem 43: 342-5 (2000)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10669559

Protease inhibitors: current status and future prospects.

J Med Chem 43: 305-41 (2000)

University of Queensland

2D 3D TSV

180

10662686

Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs.

Chem Biol 7: 27-38 (2000)

University of California San Francisco

2D 3D TSV

10658583

Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: a lead HIV protease inhibitor.

Bioorg Med Chem 7: 2775-800 (1999)

Parke-Davis Pharmaceutical Research

2D 3D TSV

10654414

DNA polymerase beta inhibitors from Tetracera boiviniana.

J Nat Prod 62: 1660-3 (2000)

University of Virginia

2D 3D TSV

10654412

DNA polymerase beta inhibitors from Baeckea gunniana.

J Nat Prod 62: 1624-6 (2000)

University of Virginia

2D 3D TSV

10650073

Dimerization of resveratrol by the grapevine pathogen Botrytis cinerea.

J Nat Prod 63: 29-33 (2000)

University of Louisiana at Monroe

2D 3D TSV

10649985

Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes.

J Med Chem 43: 292-300 (2000)

Università degli Studi

2D 3D TSV

390

10649982

A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.

J Med Chem 43: 270-7 (2000)

Universitá di Bari

2D 3D TSV

10649980

N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor.

J Med Chem 43: 250-60 (2000)

Universit£ di Camerino

2D 3D TSV

10649979

Secondary amides of (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase.

J Med Chem 43: 236-49 (2000)

Novartis Institute for Biomedical Research

2D 3D TSV

10649977

Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.

J Med Chem 43: 214-23 (2000)

Rhône-Poulenc Rorer

2D 3D TSV

10649976

Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands.

J Med Chem 43: 205-13 (2000)

Massachusetts General Hospital

2D 3D TSV

10649973

3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives.

J Med Chem 43: 177-89 (2000)

Otsuka Pharmaceutical Co., Ltd

2D 3D TSV

10649972

Antitumor agents. 199. Three-dimensional quantitative structure-activity relationship study of the colchicine binding site ligands using comparative molecular field analysis.

J Med Chem 43: 167-76 (2000)

University of North Carolina at Chapel Hill

2D 3D TSV

104

10649971

Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors.

J Med Chem 43: 156-66 (2000)

Parke-Davis Pharmaceutical Research

2D 3D TSV

180

10649969

Synthesis and pharmacological characterization of [(125)I]iodomethyllycaconitine ([(125)I]iodo-MLA). A new ligand for the alpha(7) nicotinic acetylcholine receptor.

J Med Chem 43: 142-5 (2000)

Research Triangle Institute

2D 3D TSV

10649968

Structural determinants of efficacy for kappa opioid receptors in the orvinol series: 7,7-spiro analogues of buprenorphine.

J Med Chem 43: 139-41 (2000)

University of Bristol

2D 3D TSV

10648470

Drug- and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver.

Gastroenterology 118: 422-30 (2000)

University Hospital

2D 3D TSV

10646498

Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.

J Neurochem 74: 478-89 (2000)

Janssen Research Foundation

2D 3D TSV

10644574

A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane.

Am J Physiol Gastrointest Liver Physiol 278: 156-64 (2000)

Deutsches Krebsforschungszentrum

2D 3D TSV

10639289

Synthesis and biological evaluation of dihydrobenzofuran lignans and related compounds as potential antitumor agents that inhibit tubulin polymerization.

J Med Chem 42: 5475-81 (2000)

University of Antwerp

2D 3D TSV

10639288

Tyrosine kinase inhibitors. 16. 6,5,6-tricyclic benzothieno[3, 2-d]pyrimidines and pyrimido[5,4-b-] and -[4,5-b]indoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase.

J Med Chem 42: 5464-74 (1999)

Parke-Davis Pharmaceutical Research

2D 3D TSV

10639287

Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.

J Med Chem 42: 5455-63 (2000)

National Institute of Diabetes and Digestive and Kidney Diseases

2D 3D TSV

10639286

Inhibition of Trypanosoma cruzi trypanothione reductase by acridines: kinetic studies and structure-activity relationships.

J Med Chem 42: 5448-54 (2000)

Heidelberg University

2D 3D TSV

10639285

2-(diethylamino)thieno1,3??xazin-4-ones as stable inhibitors of human leukocyte elastase.

J Med Chem 42: 5437-47 (2000)

University of Leipzig

2D 3D TSV

10639284

Design, synthesis, and biological evaluation of matrix metalloproteinase inhibitors derived from a modified proline scaffold.

J Med Chem 42: 5426-36 (2000)

University of Florida

2D 3D TSV

119

10639283

Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.

J Med Chem 42: 5415-25 (2000)

Berlex Biosciences

2D 3D TSV

135

10639281

Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity.

J Med Chem 42: 5390-401 (2000)

Universit¿a di Perugia

2D 3D TSV

10639280

Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.

J Med Chem 42: 5369-89 (1999)

AstraZeneca

2D 3D TSV

101

10639279

Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective delta-opioid receptor nonpeptide agonist ligand.

J Med Chem 42: 5359-68 (2000)

The University of Arizona

2D 3D TSV

10639276

Molecular recognition of modified adenine nucleotides by the P2Y(1)-receptor. 1. A synthetic, biochemical, and NMR approach.

J Med Chem 42: 5325-37 (2000)

Bar-Ilan University

2D 3D TSV

10639274

Synthesis and structure-activity relationships of new 1, 3-disubstituted cyclohexanes as structurally rigid leukotriene B(4) receptor antagonists.

J Med Chem 42: 5289-310 (1999)

CNRS 5074

2D 3D TSV

10639181

Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.

Proc Natl Acad Sci U S A 97: 925-30 (2000)

Vanderbilt University School of Medicine

2D 3D TSV

10636865

beta-lactam antibiotics as substrates for OCTN2, an organic cation/carnitine transporter.

J Biol Chem 275: 1699-707 (2000)

Medical College of Georgia

2D 3D TSV

10636251

Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.

Bioorg Med Chem Lett 10: 87-90 (2000)

Institute

2D 3D TSV

10636250

Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.

Bioorg Med Chem Lett 10: 83-5 (2000)

3-Dimensional Pharmaceuticals Inc

2D 3D TSV

10636249

Structure-activity and crystallographic analysis of a new class of non-amide-based thrombin inhibitor.

Bioorg Med Chem Lett 10: 79-82 (2000)

3-Dimensional Pharmaceuticals Inc

2D 3D TSV

10636248

Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors.

Bioorg Med Chem Lett 10: 75-8 (2000)

University Hospital Zurich

2D 3D TSV

10636247

New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.

Bioorg Med Chem Lett 10: 71-4 (2000)

Janssen Research Foundation

2D 3D TSV

10636245

Role of the hydrophobic moiety of tumor promoters. Synthesis and activity of 2-alkylated benzolactams.

Bioorg Med Chem Lett 10: 63-6 (2000)

University of Tokyo

2D 3D TSV

10636243

Synthesis and binding studies of some epibatidine analogues.

Bioorg Med Chem Lett 10: 55-8 (2000)

Institute of Pharmacy and Biochemistry

2D 3D TSV

10636238

Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: novel PDE4 inhibitors.

Bioorg Med Chem Lett 10: 35-8 (2000)

Institut de Recherche Jouveinal-Parke Davis

2D 3D TSV

10636237

The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family.

Bioorg Med Chem Lett 10: 31-4 (2000)

ChemBridge Corporation

2D 3D TSV

10636235

Binding dynamics of two water molecules constrained within the scytalone dehydratase binding pocket.

Bioorg Med Chem Lett 10: 23-6 (2000)

FMC Stine Research Center

2D 3D TSV

10636233

A sigma-1 receptor selective analogue of BD1008. A potential substitute for (+)-opioids in sigma receptor binding assays.

Bioorg Med Chem Lett 10: 17-8 (2000)

University of Maryland

2D 3D TSV

10636232

Design, synthesis and structure-activity relationship of a series of arginine aldehyde factor Xa inhibitors. Part 1: structures based on the (D)-Arg-Gly-Arg tripeptide sequence.

Bioorg Med Chem Lett 10: 13-6 (2000)

COR Therapeutics Inc

2D 3D TSV

10636230

Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues.

Bioorg Med Chem Lett 10: 5-8 (2000)

Merck Research Laboratories

2D 3D TSV

10636229

Amidinohydrazones as guanidine bioisosteres: application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors.

Bioorg Med Chem Lett 10: 1-4 (2000)

3-Dimensional Pharmaceuticals Inc

2D 3D TSV

10634944

The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.

Biochim Biophys Acta 1483: 285-93 (2000)

Merck Frosst Centre for Therapeutic Research

2D 3D TSV

215

10633045

Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase.

J Med Chem 43: 133-8 (2000)

Glaxo Wellcome Inc.

2D 3D TSV

10633043

Synthesis and SAR of 4-aryl-2-hydroxy-4-oxobut-2-enoic acids and esters and 2-amino-4-aryl-4-oxobut-2-enoic acids and esters: potent inhibitors of kynurenine-3-hydroxylase as potential neuroprotective agents.

J Med Chem 43: 123-7 (2000)

Glaxo Wellcome Research and Development

2D 3D TSV

10633042

Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.

J Med Chem 43: 114-22 (2000)

Harvard Medical School

2D 3D TSV

10633039

Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.

J Med Chem 43: 71-95 (2000)

University of Wisconsin-Milwaukee

2D 3D TSV

718

10633038

QSAR analysis of Delta(8)-THC analogues: relationship of side-chain conformation to cannabinoid receptor affinity and pharmacological potency.

J Med Chem 43: 59-70 (2000)

Research Triangle Institute

2D 3D TSV

10633037

Disubstituted indazoles as potent antagonists of the integrin alpha(v)beta(3).

J Med Chem 43: 41-58 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10633036

Isoxazolines as potent antagonists of the integrin alpha(v)beta(3).

J Med Chem 43: 27-40 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10633035

Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.

J Med Chem 43: 22-6 (2000)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10633034

Selective plasma hydrolysis of glucocorticoid gamma-lactones and cyclic carbonates by the enzyme paraoxonase: an ideal plasma inactivation mechanism.

J Med Chem 43: 19-21 (2000)

Glaxo Wellcome Research and Development

2D 3D TSV

10632067

Dual-site binding of bivalent 4-aminopyridine- and 4-aminoquinoline-based AChE inhibitors: contribution of the hydrophobic alkylene tether to monomer and dimer affinities.

Bioorg Med Chem 7: 2569-75 (1999)

Hong Kong University of Science and Technology

2D 3D TSV

10632058

Hydrophobic benzoic acids as inhibitors of influenza neuraminidase.

Bioorg Med Chem 7: 2487-97 (1999)

University of Alabama at Birmingham

2D 3D TSV

10617681

Possible role of valvular serotonin 5-HT(2B) receptors in the cardiopathy associated with fenfluramine.

Mol Pharmacol 57: 75-81 (2000)

DuPont Pharmaceuticals Company

2D 3D TSV

10617091

Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates.

Bioorg Med Chem Lett 9: 3459-64 (2000)

Corvas International Inc

2D 3D TSV

10617088

Synthesis and biological activities of position one and three transposed analogs of the opioid peptide YKFA.

Bioorg Med Chem Lett 9: 3441-6 (2000)

University of Louisville

2D 3D TSV

10617086

Delta opioid binding selectivity of 3-ether analogs of naltrindole.

Bioorg Med Chem Lett 9: 3435-8 (2000)

National Institute of Diabetes

2D 3D TSV

10617082

N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.

Bioorg Med Chem Lett 9: 3411-6 (2000)

Institute

2D 3D TSV

10617079

Tokaramide A, a new cathepsin B inhibitor from the marine sponge Theonella aff. mirabilis.

Bioorg Med Chem Lett 9: 3397-402 (1999)

The University of Tokyo

2D 3D TSV

10612603

Reversal of resistance in multidrug resistance protein (MRP1)-overexpressing cells by LY329146.

Bioorg Med Chem Lett 9: 3381-6 (2000)

Eli Lilly and Company

2D 3D TSV

10612602

Synthesis and opiate receptor binding properties of 17-methyl-6,7-dehydro-3,14-dihydroxy-4,5alpha-epoxy-6,7:4',5'-pyrimidin omorphinans.

Bioorg Med Chem Lett 9: 3375-80 (2000)

University of Illinois at Chicago

2D 3D TSV

10612601

4-Hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl]piperidines: selective h5-HT1D agonists for the treatment of migraine.

Bioorg Med Chem Lett 9: 3369-74 (2000)

Merck Sharp & Dohme Research Laboratories

2D 3D TSV

10612600

First fatty acylated dipeptides to affect muscarinic receptor ligand binding.

Bioorg Med Chem Lett 9: 3363-8 (2000)

University of Toledo

2D 3D TSV

10612598

4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.

Bioorg Med Chem Lett 9: 3351-6 (2000)

Celltech Therapeutics Limited

2D 3D TSV

10612597

Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.

Bioorg Med Chem Lett 9: 3347-50 (2000)

Research Triangle Institute

2D 3D TSV

10612594

Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.

Bioorg Med Chem Lett 9: 3329-34 (2000)

Glaxo Wellcome Research and Development

2D 3D TSV

10612593

N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter.

Bioorg Med Chem Lett 9: 3325-8 (2000)

Georgetown University Medical Center

2D 3D TSV

10612590

Synthesis and biological activities of NB-506 analogues: Effects of the positions of two hydroxyl groups at the indole rings.

Bioorg Med Chem Lett 9: 3307-12 (2000)

Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories

2D 3D TSV

10612589

Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.

Bioorg Med Chem Lett 9: 3301-6 (2000)

Merck Research Laboratories

2D 3D TSV

10612586

Syntheses and evaluation of amidinobenzofuran derivatives as tryptase inhibitors.

Bioorg Med Chem Lett 9: 3285-90 (2000)

Yoshitomi Pharmaceutical Industries Ltd

2D 3D TSV

10612585

Synthesis and acetylcholinesterase inhibitory activity of huperzine A-E2020 combined compound.

Bioorg Med Chem Lett 9: 3279-84 (2000)

Institute of Materia Medica

2D 3D TSV

10612583

Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine.

Bioorg Med Chem Lett 9: 3273-6 (2000)

University of New Orleans

2D 3D TSV

10612582

Blockers of human T cell Kv1.3 potassium channels using de novo ligand design and solid-phase parallel combinatorial chemistry.

Bioorg Med Chem Lett 9: 3267-72 (2000)

University of California

2D 3D TSV

10611640

Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors.

Synapse 35: 144-50 (2000)

Albany Medical College

2D 3D TSV

10611634

Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states.

Synapse 35: 79-95 (2000)

Institut de Recherches Servier

2D 3D TSV

10606521

Equilibrium thermodynamics of a physiologically-relevant heme-protein complex.

Biochemistry 38: 16876-81 (1999)

University of North Carolina at Chapel Hill

2D 3D TSV

10604951

Novel structure having antagonist actions at both the glycine site of the N-methyl-D-aspartate receptor and neuronal voltage-sensitive sodium channels: biochemical, electrophysiological, and behavioral characterization.

J Pharmacol Exp Ther 292: 215-27 (2000)

University of Colorado

2D 3D TSV

10602711

Vasorelaxation by new hybrid compounds containing dihydropyridine and pinacidil-like moieties.

J Med Chem 42: 5266-71 (1999)

National Academy of Sciences of Ukraine

2D 3D TSV

10602710

Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.

J Med Chem 42: 5254-65 (2000)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10602709

Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.

J Med Chem 42: 5241-53 (2000)

Bristol-Myers Squibb Pharmaceutical Research Institute

2D 3D TSV

10602705

Investigation of subsite preferences in aminopeptidase A (EC 3.4.11.7) led to the design of the first highly potent and selective inhibitors of this enzyme.

J Med Chem 42: 5197-211 (2000)

University of Paris

2D 3D TSV

10602703

A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.

J Med Chem 42: 5181-7 (2000)

Warner-Lambert Company

2D 3D TSV

10602702

Simple linear QSAR models based on quantum similarity measures.

J Med Chem 42: 5169-80 (2000)

Czech Academy of Sciences

2D 3D TSV

10602699

Binding constants of neuraminidase inhibitors: An investigation of the linear interaction energy method.

J Med Chem 42: 5142-52 (2000)

University of Southampton

2D 3D TSV

10602697

Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.

J Med Chem 42: 5120-30 (1999)

SUGEN, Inc.

2D 3D TSV

10602693

Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents.

J Med Chem 42: 5077-94 (2000)

Wyeth-Ayerst Research

2D 3D TSV

10602691

Alpha(2) adrenoceptor agonists as potential analgesic agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles.

J Med Chem 42: 5064-71 (1999)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10602690

Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397).

J Med Chem 42: 5061-3 (2000)

Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories

2D 3D TSV

10598788

Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.

Naunyn Schmiedebergs Arch Pharmacol 360: 488-99 (1999)

Novartis Pharma AG

2D 3D TSV

305

10585536

Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays.

Eur J Pharmacol 383: 209-14 (1999)

Hungarian Academy of Sciences

2D 3D TSV

10585212

Oxygenated analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as potential extended-action cocaine-abuse therapeutic agents.

J Med Chem 42: 5029-42 (2000)

National Institute of Diabetes and Digestive and Kidney Diseases

2D 3D TSV

138

10585211

Benzimidazole derivatives. 2. Synthesis and structure-activity relationships of new azabicyclic benzimidazole-4-carboxylic acid derivatives with affinity for serotoninergic 5-HT(3) receptors.

J Med Chem 42: 5020-8 (2000)

Universidad Complutense

2D 3D TSV

10585210

Further studies on the Dmt-Tic pharmacophore: hydrophobic substituents at the C-terminus endow delta antagonists to manifest mu agonism or mu antagonism.

J Med Chem 42: 5010-9 (2000)

University of Ferrara

2D 3D TSV

10585208

3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.

J Med Chem 42: 4981-5001 (2000)

Merck Sharp & Dohme Research Laboratories

2D 3D TSV

212

10585207

Improving the nicotinic pharmacophore with a series of (Isoxazole)methylene-1-azacyclic compounds: synthesis, structure-activity relationship, and molecular modeling.

J Med Chem 42: 4970-80 (1999)

Novo Nordisk A/S

2D 3D TSV

10585206

Structure-activity relationship studies of novel heteroretinoids: induction of apoptosis in the HL-60 cell line by a novel isoxazole-containing heteroretinoid.

J Med Chem 42: 4961-9 (2000)

Università di Ferrara

2D 3D TSV

10585205

On the bioactive conformation of NAN-190 (1) and MP3022 (2), 5-HT(1A) receptor antagonists.

J Med Chem 42: 4952-60 (2000)

Polish Academy of Sciences

2D 3D TSV

10580501

Kainate receptors are involved in synaptic plasticity.

Nature 402: 297-301 (1999)

University of Bristol

2D 3D TSV

10579862

Anti-HIV-1 protease triterpenoid saponins from the seeds of Aesculus chinensis.

J Nat Prod 62: 1510-3 (1999)

Beijing Medical University

2D 3D TSV

10579852

Synthesis and biological evaluation of a potent E-selectin antagonist.

J Med Chem 42: 4909-13 (1999)

Novartis Pharma AG

2D 3D TSV

10579851

New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.

J Med Chem 42: 4890-908 (1999)

AstraZeneca

2D 3D TSV

151

10579850

Fused bicyclic Gly-Asp beta-turn mimics with specific affinity for GPIIb-IIIa.

J Med Chem 42: 4875-89 (1999)

Eli Lilly and Company

2D 3D TSV

10579849

Novel modifications in the alkenyldiarylmethane (ADAM) series of non-nucleoside reverse transcriptase inhibitors.

J Med Chem 42: 4861-74 (1999)

Purdue University

2D 3D TSV

10579848

Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged diarylamine side chain.

J Med Chem 42: 4853-60 (1999)

Harvard Medical School

2D 3D TSV

10579847

Discovery of a series of cyclohexylethylamine-containing protein farnesyltransferase inhibitors exhibiting potent cellular activity.

J Med Chem 42: 4844-52 (1999)

Abbott Laboratories

2D 3D TSV

10579846

Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes.

J Med Chem 42: 4836-43 (1999)

Georgia Institute of Technology

2D 3D TSV

10579845

Synthesis, acid-base behavior, and binding properties of 6-modified myo-inositol 1,4,5-tris(phosphate)s.

J Med Chem 42: 4824-35 (1999)

Laboratoire de Pharmacochimie de la Communication Cellulaire UMR 7081 du CNRS

2D 3D TSV

10579843

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series.

J Med Chem 42: 4804-13 (1999)

Synaptic Pharmaceutical Corporation

2D 3D TSV

10579842

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.

J Med Chem 42: 4794-803 (1999)

Synaptic Pharmaceutical Corporation

2D 3D TSV

10579841

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.

J Med Chem 42: 4778-93 (1999)

Synaptic Pharmaceutical Corporation

2D 3D TSV

113

10579840

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.

J Med Chem 42: 4764-77 (1999)

Synaptic Pharmaceutical Corporation

2D 3D TSV

10579836

Synthesis and biological evaluation of the first N-alkyl cage dimeric 4-aryl-1,4-dihydropyridines as novel nonpeptidic HIV-1 protease inhibitors.

J Med Chem 42: 4729-32 (1999)

Martin-Luther-University Halle-Wittenberg

2D 3D TSV

10579835

Inhibition and substrate activity of conformationally rigid vigabatrin analogues with gamma-aminobutyric acid aminotransferase.

J Med Chem 42: 4725-8 (1999)

Northwestern University

2D 3D TSV

10579830

Discovery of novel non-peptide CCR1 receptor antagonists.

J Med Chem 42: 4680-94 (1999)

Berlex Biosciences

2D 3D TSV

10579829

Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation.

J Med Chem 42: 4669-79 (1999)

Westfälische Wilhelms-Universität Münster

2D 3D TSV

10579828

5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.

J Med Chem 42: 4659-68 (1999)

Insituto de Qu�mica M�dica (CSIC), Juan de la Cierva 3, E-28006 Madrid, Spain.

2D 3D TSV

10579825

Structural specificity of chloroquine-hematin binding related to inhibition of hematin polymerization and parasite growth.

J Med Chem 42: 4630-9 (1999)

University of Nebraska Medical Center

2D 3D TSV

10579824

Asymmetric synthesis of 9-alkyl-2-benzyl-6,7-benzomorphans: characterization as novel sigma receptor ligands.

J Med Chem 42: 4621-9 (1999)

Research Triangle Institute

2D 3D TSV

10579821

Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.

J Med Chem 42: 4584-603 (1999)

Novartis Horsham Research Centre

2D 3D TSV

10579820

Specific nonpeptide photoprobes as tools for the structural study of the angiotensin II AT(1) receptor.

J Med Chem 42: 4572-83 (1999)

Laboratoires Fournier S.A.

2D 3D TSV

10579818

Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.

J Med Chem 42: 4547-62 (1999)

Procter and Gamble Pharmaceuticals

2D 3D TSV

162

10579817

Molecular modeling studies on G-quadruplex complexes of telomerase inhibitors: structure-activity relationships.

J Med Chem 42: 4538-46 (1999)

The Institute of Cancer Research

2D 3D TSV

10579816

Angiotensin II analogues encompassing 5,9- and 5,10-fused thiazabicycloalkane tripeptide mimetics.

J Med Chem 42: 4524-37 (1999)

Uppsala University

2D 3D TSV

10579815

Affinity and selectivity of matrix metalloproteinase inhibitors: a chemometrical study from the perspective of ligands and proteins.

J Med Chem 42: 4506-23 (1999)

Hoechst Marion Roussel Inc

2D 3D TSV

168

10579811

Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.

J Med Chem 42: 4473-8 (1999)

Università degli Studi di Ferrara

2D 3D TSV

10578127

Effects of glibenclamide on glycylsarcosine transport by the rat peptide transporters PEPT1 and PEPT2.

Br J Pharmacol 128: 1159-64 (1999)

Kyoto University Hospital

2D 3D TSV

10576696

Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands.

Bioorg Med Chem Lett 9: 3243-8 (1999)

Merck

2D 3D TSV

10576693

Dicationic 2-fluorenonylcarbapenems: potent anti-MRS agents with improved solubility and pharmacokinetic properties.

Bioorg Med Chem Lett 9: 3225-30 (1999)

Merck Research Laboratories

2D 3D TSV

10576692

Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).

Bioorg Med Chem Lett 9: 3221-4 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10576691

Unsymmetrical cyclic ureas as HIV-1 protease inhibitors: novel biaryl indazoles as P2/P2' substituents.

Bioorg Med Chem Lett 9: 3217-20 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10576690

Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine.

Bioorg Med Chem Lett 9: 3211-6 (1999)

Georgetown University Medical Center

2D 3D TSV

10576685

Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.

Bioorg Med Chem Lett 9: 3187-92 (1999)

Merck Frosst Centre for Therapeutic Research

2D 3D TSV

10576684

A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.

Bioorg Med Chem Lett 9: 3181-6 (1999)

Merck Frosst Centre for Therapeutic Research

2D 3D TSV

10571174

(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.

Bioorg Med Chem Lett 9: 3053-6 (1999)

Research Triangle Institute

2D 3D TSV

10571170

Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.

Bioorg Med Chem Lett 9: 3031-4 (1999)

Dipartimento di Scienze Farmaceutiche - Università di Genova

2D 3D TSV

10571165

Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70.

Bioorg Med Chem Lett 9: 3009-14 (1999)

ARIAD Pharmaceuticals Inc

2D 3D TSV

10571163

A novel class of Na+ and Ca2+ channel dual blockers with highly potent anti-ischemic effects.

Bioorg Med Chem Lett 9: 2999-3002 (1999)

Institute for Bio-Medical Research

2D 3D TSV

10571156

Synthesis and biological characterization of sqbazide, a novel biotinylated photoaffinity probe for the study of the human platelet thromboxane A2 receptor.

Bioorg Med Chem Lett 9: 2963-8 (1999)

Ecole Nationale Supérieure de Chimie de Paris

2D 3D TSV

10571154

Guanidine-substituted imidazoles as inhibitors of nitric oxide synthase.

Bioorg Med Chem Lett 9: 2953-8 (1999)

Wake Forest University Winston-Salem

2D 3D TSV

10571147

Mapping the X(+1) binding site of the Grb2-SH2 domain with alpha,alpha-disubstituted cyclic alpha-amino acids.

Bioorg Med Chem Lett 9: 2915-20 (1999)

Novartis Pharma Inc

2D 3D TSV

10571146

3-Acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid as novel vanilloid receptor agonists.

Bioorg Med Chem Lett 9: 2909-14 (1999)

Seoul National University

2D 3D TSV

10570053

Selectivity of the polyspecific cation transporter rOCT1 is changed by mutation of aspartate 475 to glutamate.

Mol Pharmacol 56: 1254-61 (1999)

Bayerische Julius-Maximilians-Universit£t

2D 3D TSV

10570049

Effect of multidrug resistance-reversing agents on transporting activity of human canalicular multispecific organic anion transporter.

Mol Pharmacol 56: 1219-28 (1999)

Kagoshima University

2D 3D TSV

10565848

Characterization and function of the bovine kidney epithelial angiotensin receptor subtype 4 using angiotensin IV and divalinal angiotensin IV as receptor ligands.

J Pharmacol Exp Ther 291: 1242-9 (1999)

Washington State University

2D 3D TSV

10565843

Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity.

J Pharmacol Exp Ther 291: 1204-9 (1999)

Vanderbilt University School of Medicine

2D 3D TSV

10565829

Ring-constrained orvinols as analogs of buprenorphine: differences in opioid activity related to configuration of C(20) hydroxyl group.

J Pharmacol Exp Ther 291: 1093-9 (1999)

Loughborough University

2D 3D TSV

10560746

Revised structure of a homonojirimycin isomer from Aglaonema treubii: first example of a naturally occurring alpha-homoallonojirimycin.

Bioorg Med Chem Lett 9: 3171-4 (1999)

Institut de Chimie Organique et Analytique (I.C.O.A.)

2D 3D TSV

10560745

Selective inhibition of low affinity IgE receptor (CD23) processing: P1' bicyclomethyl substituents.

Bioorg Med Chem Lett 9: 3165-70 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10560742

3-Amidinophenylalanine-based inhibitors of urokinase.

Bioorg Med Chem Lett 9: 3147-52 (1999)

Universität Jena

2D 3D TSV

10560741

Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.

Bioorg Med Chem Lett 9: 3143-6 (1999)

Friedrich-Alexander University

2D 3D TSV

10560740

The inhibition of human cytomegalovirus (hCMV) protease by hydroxylamine derivatives.

Bioorg Med Chem Lett 9: 3137-42 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10560733

4-Chlorobenzyl sulfonamide and sulfamide derivatives of histamine homologues: the design of potent histamine H3 receptor antagonists.

Bioorg Med Chem Lett 9: 3103-8 (1999)

The James Black Foundation

2D 3D TSV

10560731

Aminomethyl-2,6-difluorophenols as a novel class of increased lipophilicity GABA(C) receptor antagonists.

Bioorg Med Chem Lett 9: 3093-8 (1999)

The University of Sydney

2D 3D TSV

10543913

Isolation of xestosterol esters of brominated acetylenic fatty acids from the marine sponge xestospongia testudinaria

J Nat Prod 62: 1439-42 (1999)

Griffith University

2D 3D TSV

10543890

Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.

J Med Chem 42: 4462-70 (1999)

Universita' degli Studi di Salerno

2D 3D TSV

10543889

Retention of immunosuppressant activity in an ascomycin analogue lacking a hydrogen-bonding interaction with FKBP12.

J Med Chem 42: 4456-61 (1999)

Abbott Laboratories

2D 3D TSV

10543888

Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.

J Med Chem 42: 4446-55 (1999)

National Institute on Drug Abuse-Intramural Research Program

2D 3D TSV

10543887

Heteroarotinoids inhibit head and neck cancer cell lines in vitro and in vivo through both RAR and RXR retinoic acid receptors.

J Med Chem 42: 4434-45 (1999)

University of Oklahoma Health Sciences Center

2D 3D TSV

10543886

Two-stage method for protein-ligand docking.

J Med Chem 42: 4422-33 (1999)

German National Research Center for Information Technology

2D 3D TSV

10543883

Evaluation and biological properties of reactive ligands for the mapping of the glycine site on the N-methyl-D-aspartate (NMDA) receptor.

J Med Chem 42: 4394-404 (1999)

Université Louis Pasteur

2D 3D TSV

10543881

Compounds that activate the mouse melanocortin-1 receptor identified by screening a small molecule library based upon the beta-turn.

J Med Chem 42: 4380-7 (1999)

Oregon Health Sciences University

2D 3D TSV

10543880

Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.

J Med Chem 42: 4362-79 (1999)

Universita' degli Studi di Salerno

2D 3D TSV

10543879

Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.

J Med Chem 42: 4351-61 (1999)

University of Kansas

2D 3D TSV

10543877

Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.

J Med Chem 42: 4331-42 (1999)

Uppsala University

2D 3D TSV

10543874

Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase.

J Med Chem 42: 4300-12 (1999)

Cardiff University

2D 3D TSV

10543872

Synthesis of novel GABA uptake inhibitors. 4. Bioisosteric transformation and successive optimization of known GABA uptake inhibitors leading to a series of potent anticonvulsant drug candidates.

J Med Chem 42: 4281-91 (1999)

Novo Nordisk A/S

2D 3D TSV

10531324

Thermodynamic analyses reveal role of water release in epitope recognition by a monoclonal antibody against the human guanylyl cyclase C receptor.

J Biol Chem 274: 31272-8 (1999)

Indian Institute of Science

2D 3D TSV

10530956

Structure-activity relationship of HIV-1 protease inhibitors containing alpha-hydroxy-beta-amino acids. Detailed study of P1 site.

Bioorg Med Chem 7: 2063-72 (1999)

Sankyo Co., Ltd

2D 3D TSV

10525090

Recognition of L-amino acid ester compounds by rat peptide transporters PEPT1 and PEPT2.

J Pharmacol Exp Ther 291: 705-9 (1999)

Kyoto University Hospital

2D 3D TSV

10522712

The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors.

Bioorg Med Chem Lett 9: 2887-92 (1999)

British Biotech Pharmaceuticals Limited

2D 3D TSV

109

10522707

2-chloro-3-substituted-1,4-naphthoquinone inactivators of human cytomegalovirus protease.

Bioorg Med Chem Lett 9: 2863-6 (1999)

GlaxoWellcome Medicines Research Centre

2D 3D TSV

10522706

Interaction of tyrosyl aryl dipeptides with S. aureus tyrosyl tRNA synthetase: inhibition and crystal structure of a complex.

Bioorg Med Chem Lett 9: 2859-62 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10522703

Design and synthesis of novel dihydropyridine alpha-1a antagonists.

Bioorg Med Chem Lett 9: 2843-8 (1999)

Synaptic Pharmaceutical Corporation

2D 3D TSV

103

10522702

Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors.

Bioorg Med Chem Lett 9: 2837-42 (1999)

NV Organon

2D 3D TSV

10522701

Synthesis and biological evaluation of 1,1-difluoro-2-(tetrahydro-3-furanyl)ethylphosphonic acids possessing a N9-purinylmethyl functional group at the ring. a new class of inhibitors for purine nucleoside phosphorylases.

Bioorg Med Chem Lett 9: 2833-6 (1999)

Tokyo University of Pharmacy & Life Science

2D 3D TSV

10522699

Design, combinatorial chemical synthesis and in vitro characterization of novel urea based gelatinase inhibitors.

Bioorg Med Chem Lett 9: 2823-6 (1999)

University of Wisconsin-Madison

2D 3D TSV

10522698

Synthesis and pharmacological profile of 1-aryl-3-substituted pyrrolo[3,2-c]quinolines.

Bioorg Med Chem Lett 9: 2819-22 (1999)

Korea Research Institute of Chemical Technology

2D 3D TSV

10522697

Discovery of subtype-selective NMDA receptor ligands: 4-benzyl-1-piperidinylalkynylpyrroles, pyrazoles and imidazoles as NR1A/2B antagonists.

Bioorg Med Chem Lett 9: 2815-8 (1999)

Warner-Lambert Company

2D 3D TSV

10522696

Stereospecific synthesis of a GS 4104 metabolite: determination of absolute stereochemistry and influenza neuraminidase inhibitory activity.

Bioorg Med Chem Lett 9: 2811-4 (1999)

Gilead Sciences Inc

2D 3D TSV

10522695

Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.

Bioorg Med Chem Lett 9: 2805-10 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10522694

The synthesis of a new class of oxytocin antagonists.

Bioorg Med Chem Lett 9: 2801-4 (1999)

Ferring Research Institute Inc.

2D 3D TSV

10522693

Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors.

Bioorg Med Chem Lett 9: 2795-800 (1999)

Institute of Science and Technology

2D 3D TSV

10514305

Novel and known constituents from Buddleja species and their activity against leukocyte eicosanoid generation.

J Nat Prod 62: 1241-5 (1999)

Peking Union Medical College and Chinese Academy of Medical Sciences

2D 3D TSV

10514298

Novel partial agonists for the histamine H(3) receptor with high in vitro and in vivo activity.

J Med Chem 42: 4269-74 (1999)

Freie Universität Berlin

2D 3D TSV

10514296

Further studies on oxygenated tryptamines with LSD-like activity incorporating a chiral pyrrolidine moiety into the side chain.

J Med Chem 42: 4257-63 (1999)

Purdue University

2D 3D TSV

10514295

3-Alkyl-6-chloro-2-pyrones: selective inhibitors of pancreatic cholesterol esterase.

J Med Chem 42: 4250-6 (1999)

University of New Mexico

2D 3D TSV

10514294

Synthesis of a series of 4-benzyloxyaniline analogues as neuronal N-type calcium channel blockers with improved anticonvulsant and analgesic properties.

J Med Chem 42: 4239-49 (1999)

Warner-Lambert Company

2D 3D TSV

10514293

Selective A(3) adenosine receptor antagonists: water-soluble 3, 5-diacyl-1,2,4-trialkylpyridinium salts and their oxidative generation from dihydropyridine precursors.

J Med Chem 42: 4232-8 (1999)

National Institute of Diabetes

2D 3D TSV

10514292

Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions.

J Med Chem 42: 4225-31 (1999)

Hong Kong University of Science and Technology

2D 3D TSV

10514291

J Med Chem 42: 4214-24 (1999)

University of Bologna

2D 3D TSV

10514289

Synthesis and characterization of bradykinin B(2) receptor agonists containing constrained dipeptide mimics.

J Med Chem 42: 4193-201 (1999)

University of Montpellier

2D 3D TSV

10514288

Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.

J Med Chem 42: 4185-92 (1999)

University of Montpellier

2D 3D TSV

10514285

Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.

J Med Chem 42: 4150-60 (1999)

Medivir AB

2D 3D TSV

10514284

Synthesis and structure-activity relationships of the (alkylamino)piperidine-containing BHAP class of non-nucleoside reverse transcriptase inhibitors: effect of 3-alkylpyridine ring substitution.

J Med Chem 42: 4140-9 (1999)

Pharmacia & Upjohn

2D 3D TSV

10514283

Protein kinase C ligands based on tetrahydrofuran templates containing a new set of phorbol ester pharmacophores.

J Med Chem 42: 4129-39 (1999)

Seoul National University

2D 3D TSV

10514281

Inhibition of neuronal nitric oxide synthase by 4-amino pteridine derivatives: structure-activity relationship of antagonists of (6R)-5,6,7,8-tetrahydrobiopterin cofactor.

J Med Chem 42: 4108-21 (1999)

Julius-Maximilians University Würzburg

2D 3D TSV

10514279

Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70.

J Med Chem 42: 4088-98 (1999)

ARIAD Pharmaceuticals Inc

2D 3D TSV

145

10514278

Antitumor agents. 196. Substituted 2-thienyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.

J Med Chem 42: 4081-7 (1999)

University of North Carolina at Chapel Hill

2D 3D TSV

10514275

Inhibitors of the C(2)-symmetric HIV-1 protease: nonsymmetric binding of a symmetric cyclic sulfamide with ketoxime groups in the P2/P2' side chains.

J Med Chem 42: 4054-61 (1999)

Uppsala University

2D 3D TSV

10514271

Diethylcarbamoylating/nitroxylating agents as dual action inhibitors of aldehyde dehydrogenase: a disulfiram-cyanamide merger.

J Med Chem 42: 4016-20 (1999)

VA Medical Center

2D 3D TSV

10509933

Discovery of CP-199,330 and CP-199,331: two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity.

Bioorg Med Chem Lett 9: 2773-8 (1999)

Pfizer Inc

2D 3D TSV

10509931

Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin.

Bioorg Med Chem Lett 9: 2763-6 (1999)

University of Arizona

2D 3D TSV

10509929

Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.

Bioorg Med Chem Lett 9: 2753-8 (1999)

Rhône-Poulenc Rorer

2D 3D TSV

116

10509928

Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework.

Bioorg Med Chem Lett 9: 2747-52 (1999)

Abbott Laboratories

2D 3D TSV

10509927

Structure-activity relationships of biphenyl tetrazoles as metallo-beta-lactamase inhibitors.

Bioorg Med Chem Lett 9: 2741-6 (1999)

Merck Research Laboratories

2D 3D TSV

10509926

9-[(2'S,3'S)-3'-formyl-2',3'-dihydroxypropyl]adenine: a facile affinity-labeling probe of human S-adenosyl-L-homocysteine hydrolase.

Bioorg Med Chem Lett 9: 2737-40 (1999)

Gifu University

2D 3D TSV

10509923

N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.

Bioorg Med Chem Lett 9: 2721-6 (1999)

Institute

2D 3D TSV

10509922

Heterocyclic analogues of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor.

Bioorg Med Chem Lett 9: 2715-20 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10509919

New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor.

Bioorg Med Chem Lett 9: 2699-704 (1999)

Merck Frosst Centre for Therapeutic Research

2D 3D TSV

103

10509910

Syntheses of novel antitumor dihydroxanthone derivatives with inhibitory activity against DNA topoisomerase II.

Bioorg Med Chem Lett 9: 2653-6 (1999)

Ajinomoto Co. Inc

2D 3D TSV

10508448

Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.

J Med Chem 42: 4001-9 (1999)

Brown University

2D 3D TSV

10508446

Axially chiral 1,7-naphthyridine-6-carboxamide derivatives as orally active tachykinin NK(1) receptor antagonists: synthesis, antagonistic activity, and effects on bladder functions.

J Med Chem 42: 3982-93 (1999)

Takeda Chemical Industries, Ltd

2D 3D TSV

10508445

Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-azamacrocycles that inhibit HIV-1 and HIV-2 replication by antagonism of the chemokine receptor CXCR4.

J Med Chem 42: 3971-81 (1999)

AnorMED Inc.

2D 3D TSV

10508444

Synthesis and SAR of 1-alkyl-2-phenylethylamine derivatives designed from N,N-dipropyl-4-methoxy-3-(2-phenylethoxy)phenylethylamine to discover sigma(1) ligands.

J Med Chem 42: 3965-70 (1999)

Taisho Pharmaceutical Company Ltd

2D 3D TSV

10508441

Novel 2-phenylimidazo[1,2-a]pyridine derivatives as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity, and in vivo studies.

J Med Chem 42: 3934-41 (1999)

Universit£ degli Studi di Bari

2D 3D TSV

10508439

Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations.

J Med Chem 42: 3910-8 (1999)

Washington University

2D 3D TSV

10508435

Substituted isoquinolines and quinazolines as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor alpha.

J Med Chem 42: 3860-73 (1999)

University of California

2D 3D TSV

10508434

Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis.

J Med Chem 42: 3852-9 (1999)

Abbott Laboratories

2D 3D TSV

10508432

Design and fast synthesis of C-terminal duplicated potent C(2)-symmetric P1/P1'-modified HIV-1 protease inhibitors.

J Med Chem 42: 3835-44 (1999)

Uppsala University

2D 3D TSV

10508430

Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors.

J Med Chem 42: 3809-20 (1999)

AstraZeneca

2D 3D TSV

10508429

Novel farnesol and geranylgeraniol analogues: A potential new class of anticancer agents directed against protein prenylation.

J Med Chem 42: 3800-8 (1999)

Parke-Davis Pharmaceutical Research

2D 3D TSV

10508427

A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.

J Med Chem 42: 3785-8 (1999)

Glaxo Wellcome Research & Development

2D 3D TSV

10508426

N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity.

J Med Chem 42: 3779-84 (1999)

Merck Research Laboratories

2D 3D TSV

10508425

Mixture-based synthetic combinatorial libraries.

J Med Chem 42: 3743-78 (1999)

Torrey Pines Institute for Molecular Studies

2D 3D TSV

10499421

The cloned guinea pig neuropeptide Y receptor Y1 conforms to other mammalian Y1 receptors.

Peptides 20: 1043-53 (1999)

Uppsala University

2D 3D TSV

10498829

Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells.

Br J Pharmacol 128: 13-20 (1999)

Cerebrus Ltd

2D 3D TSV

10498222

Asymmetric synthesis of novel quaternary alpha-hydroxy-delta-lactam dipeptide surrogates.

Bioorg Med Chem Lett 9: 2625-8 (1999)

Corvas International Inc

2D 3D TSV

10498221

Investigation of the 4-O-alkylamine substituent of non-peptide quinolone GnRH receptor antagonists.

Bioorg Med Chem Lett 9: 2621-4 (1999)

Merck Research Laboratories

2D 3D TSV

10498220

Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist.

Bioorg Med Chem Lett 9: 2615-20 (1999)

Merck Research Laboratories

2D 3D TSV

10498218

Quinoline-2,4-dicarboxylic acids: synthesis and evaluation as inhibitors of the glutamate vesicular transport system.

Bioorg Med Chem Lett 9: 2607-12 (1999)

The University of Montana

2D 3D TSV

10498215

New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.

Bioorg Med Chem Lett 9: 2593-8 (1999)

Wyeth-Ayerst Research Laboratories

2D 3D TSV

10498212

Preparation and receptor binding affinities of cyclic C-terminal neurotensin (8-13) and (9-13) analogues.

Bioorg Med Chem Lett 9: 2579-82 (1999)

Medical University of South Carolina

2D 3D TSV

10498211

Novel benzo-fused lactam scaffolds as factor Xa inhibitors.

Bioorg Med Chem Lett 9: 2573-8 (1999)

Corvas International Inc

2D 3D TSV

10498210

A new class of selective and potent inhibitors of neuronal nitric oxide synthase.

Bioorg Med Chem Lett 9: 2569-72 (1999)

Pfizer Inc

2D 3D TSV

10498208

Protein kinase C modulators bearing dicarba-CLOSO-dodecaborane as a hydrophobic pharmacophore.

Bioorg Med Chem Lett 9: 2561-4 (1999)

University of Tokyo

2D 3D TSV

10498206

Synthesis and SAR of thioester and thiol inhibitors of IMP-1 metallo-beta-lactamase.

Bioorg Med Chem Lett 9: 2549-54 (1999)

Merck Research Laboratorie

2D 3D TSV

10498204

Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.

Bioorg Med Chem Lett 9: 2539-44 (1999)

Rh£ne-Poulenc Rorer

2D 3D TSV

10498203

Dysidiolide and related gamma-hydroxy butenolide compounds as inhibitors of the protein tyrosine phosphatase, CDC25.

Bioorg Med Chem Lett 9: 2537-8 (1999)

Mitotix Inc

2D 3D TSV

10498202

Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors.

Bioorg Med Chem Lett 9: 2531-6 (1999)

Bayer Corporation

2D 3D TSV

10498200

Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.

Bioorg Med Chem Lett 9: 2521-4 (1999)

Pharmacia & Upjohn

2D 3D TSV

10498198

A new potent inhibitor of fungal melanin biosynthesis identified through combinatorial chemistry.

Bioorg Med Chem Lett 9: 2509-14 (1999)

FMC Stine Research Center

2D 3D TSV

10498197

The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2.

Bioorg Med Chem Lett 9: 2503-8 (1999)

Warner-Lambert Company

2D 3D TSV

10498196

The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.

Bioorg Med Chem Lett 9: 2497-502 (1999)

Warner-Lambert Company

2D 3D TSV

10498195

2,7-diazabicyclo[3.3.0]octanes as novel h5-HT receptor agonists.

Bioorg Med Chem Lett 9: 2491-6 (1999)

Merck Sharp & Dohme Research Laboratories

2D 3D TSV

10498193

Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.

Bioorg Med Chem Lett 9: 2483-6 (1999)

Biotech Research Institute

2D 3D TSV

10498189

Human telomerase inhibition by substituted acridine derivatives.

Bioorg Med Chem Lett 9: 2463-8 (1999)

The Institute of Cancer Research

2D 3D TSV

10496952

Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.

Mol Pharmacol 56: 705-13 (1999)

University of Virginia

2D 3D TSV

10494877

2-Substituted N-ethylcarboxamidoadenosine derivatives as high-affinity agonists at human A3 adenosine receptors.

Naunyn Schmiedebergs Arch Pharmacol 360: 103-8 (1999)

Universität W�rzburg

2D 3D TSV

10484490

Cloning of mouse prostaglandin transporter PGT cDNA: species-specific substrate affinities.

Am J Physiol 277: 734-41 (1999)

Albert Einstein College of Medicine

2D 3D TSV

10482466

7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist.

Bioorg Med Chem 7: 1743-54 (1999)

Otsuka Pharmaceutical Co., Ltd

2D 3D TSV

10480891

Salt links dominate affinity of antibody HyHEL-5 for lysozyme through enthalpic contributions.

J Biol Chem 274: 26838-42 (1999)

University of Houston

2D 3D TSV

10479344

Secobatzellines A and B, two new enzyme inhibitors from a deep-water Caribbean sponge of the genus Batzella.

J Nat Prod 62: 1208-11 (1999)

Harbor Branch Oceanographic Institution

2D 3D TSV

10479314

DNA polymerase beta inhibitors from Sandoricum koetjape.

J Nat Prod 62: 1110-3 (1999)

University of Virginia Charlottesville

2D 3D TSV

10479306

Small peptides containing phosphotyrosine and adjacent alphaMe-phosphotyrosine or its mimetics as highly potent inhibitors of Grb2 SH2 domain.

J Med Chem 42: 3737-41 (1999)

University of Paris

2D 3D TSV

10479303

Design, synthesis, and evaluation of chromen-2-ones as potent and selective human dopamine D4 antagonists.

J Med Chem 42: 3718-25 (1999)

Warner-Lambert Company

2D 3D TSV

10479301

Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy.

J Med Chem 42: 3701-10 (1999)

Abbott Laboratories

2D 3D TSV

10479300

Carbonic anhydrase inhibitors: synthesis of water-soluble, aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route.

J Med Chem 42: 3690-700 (1999)

Universit£ degli Studi

2D 3D TSV

383

10479299

Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.

J Med Chem 42: 3679-89 (1999)

Abbott Laboratories

2D 3D TSV

10479298

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.

J Med Chem 42: 3668-78 (1999)

Abbott Laboratories

2D 3D TSV

10479296

Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors.

J Med Chem 42: 3647-56 (1999)

Massachusetts General Hospital

2D 3D TSV

10479295

2-thioether 5'-O-(1-thiotriphosphate)adenosine derivatives as new insulin secretagogues acting through P2Y-Receptors.

J Med Chem 42: 3636-46 (1999)

Bar-Ilan University

2D 3D TSV

10479294

Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding.

J Med Chem 42: 3629-35 (1999)

Leiden/Amsterdam Center for Drug Research

2D 3D TSV

10479292

Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties.

J Med Chem 42: 3615-22 (1999)

Max-Planck Research Unit

2D 3D TSV

10479291

Synthesis, structure-activity relationships, and RARgamma-ligand interactions of nitrogen heteroarotinoids.

J Med Chem 42: 3602-14 (1999)

University of Oklahoma Health Sciences Center

2D 3D TSV

10479290

Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.

J Med Chem 42: 3588-601 (1999)

University of Kansas

2D 3D TSV

10479289

Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.

J Med Chem 42: 3572-87 (1999)

Rhone-Poulenc Rorer

2D 3D TSV

10479288

Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.

J Med Chem 42: 3557-71 (1999)

Rh£ne-Poulenc Rorer

2D 3D TSV

141

10479286

Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.

J Med Chem 42: 3527-38 (1999)

Southern Research Institute

2D 3D TSV

10479285

The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.

J Med Chem 42: 3520-6 (1999)

Clinical Research Institute of Montreal

2D 3D TSV

10479284

5-deazafolate analogues with a rotationally restricted glutamate or ornithine side chain: synthesis and binding interaction with folylpolyglutamate synthetase.

J Med Chem 42: 3510-9 (1999)

Harvard Medical School

2D 3D TSV

10479283

CoMFA study of novel phenyl ring-substituted 3alpha-(diphenylmethoxy)tropane analogues at the dopamine transporter.

J Med Chem 42: 3502-9 (1999)

National Institute on Drug Abuse-Intramural Research Program

2D 3D TSV

10479279

N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.

J Med Chem 42: 3463-77 (1999)

Novo Nordisk A/S

2D 3D TSV

10479278

Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents.

J Med Chem 42: 3447-62 (1999)

Novo Nordisk A/S

2D 3D TSV

10479277

Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations.

J Med Chem 42: 3436-46 (1999)

Georgetown University Medical Center

2D 3D TSV

10479275

A multisubstrate adduct inhibitor of AICAR transformylase.

J Med Chem 42: 3421-4 (1999)

The Pennsylvania State University

2D 3D TSV

10476886

Structure-activity relationship at the proximal phenyl group in a series of non-peptidyl N-type calcium channel antagonists.

Bioorg Med Chem Lett 9: 2453-8 (1999)

Parke-Davis Pharmaceutical Research

2D 3D TSV

10476885

Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers.

Bioorg Med Chem Lett 9: 2447-52 (1999)

Warner-Lambert Company

2D 3D TSV

10476884

Synthesis of a phostone glycomimetic of the endothelin converting enzyme inhibitor phosphoramidon.

Bioorg Med Chem Lett 9: 2441-6 (1999)

Université de Montréal

2D 3D TSV

10476879

Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.

Bioorg Med Chem Lett 9: 2413-8 (1999)

Cadus Pharmaceutical Corporation

2D 3D TSV

10476878

Naphthazarin derivatives (II): formation of glutathione conjugate, inhibition of DNA topoisomerase-I and cytotoxicity.

Bioorg Med Chem Lett 9: 2407-12 (1999)

Chungnam National University

2D 3D TSV

10476877

NMR-based discovery of phosphotyrosine mimetics that bind to the Lck SH2 domain.

Bioorg Med Chem Lett 9: 2403-6 (1999)

Abbott Laboratories

2D 3D TSV

10476876

Molecular structure of FR901277, a novel inhibitor of human leukocyte elastase, and its binding mode simulation.

Bioorg Med Chem Lett 9: 2397-402 (1999)

Fujisawa Pharmaceutical Co., Ltd

2D 3D TSV

10476875

Substituted indoles as potent and orally active 5-lipoxygenase activating protein (FLAP) inhibitors.

Bioorg Med Chem Lett 9: 2391-6 (1999)

Merck Frosst Center for Therapeutic Research

2D 3D TSV

10476873

Synthesis and estrogen receptor binding affinity of a porphyrin-estradiol conjugate for targeted photodynamic therapy of cancer.

Bioorg Med Chem Lett 9: 2379-84 (1999)

Boston University School of Medicine

2D 3D TSV

10476871

P2-achiral, P'-extended alpha-ketoamide inhibitors of calpain I.

Bioorg Med Chem Lett 9: 2371-4 (1999)

Cephalon Inc

2D 3D TSV

10476870

Hydroxyoxazolidines as alpha-aminoacetaldehye equivalents: novel inhibitors of calpain.

Bioorg Med Chem Lett 9: 2365-70 (1999)

Hoechst Marion Roussel Inc

2D 3D TSV

10476869

Structure-activity relationships of a novel class of Src SH2 inhibitors.

Bioorg Med Chem Lett 9: 2359-64 (1999)

ARIAD Pharmaceuticals Inc

2D 3D TSV

10476868

Structure-based design and synthesis of a novel class of Src SH2 inhibitors.

Bioorg Med Chem Lett 9: 2353-8 (1999)

ARIAD Pharmaceuticals Inc

2D 3D TSV

10476866

8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists.

Bioorg Med Chem Lett 9: 2343-8 (1999)

F. Hoffmann-La Roche Inc

2D 3D TSV

10476865

Synthesis of new (benzimidazolyl)piperazines with affinity for the 5-HT1A receptor via Pd(0) amination of bromobenzimidazoles.

Bioorg Med Chem Lett 9: 2339-42 (1999)

Universidad Complutense

2D 3D TSV

10476864

Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors.

Bioorg Med Chem Lett 9: 2335-8 (1999)

Hong Kong University of Science and Technology

2D 3D TSV

10476857

Rational herbicide design by inhibition of tryptophan biosynthesis.

Bioorg Med Chem Lett 9: 2297-302 (1999)

American Cyanamid

2D 3D TSV

10476856

A rapid method to identify exo-protease inhibitors.

Bioorg Med Chem Lett 9: 2291-6 (1999)

The Scripps Research Institute

2D 3D TSV

10471378

6-Methyl-3'-bromoflavone, a high-affinity ligand for the benzodiazepine binding site of the GABA(A) receptor with some antagonistic properties.

Biochem Biophys Res Commun 262: 643-6 (1999)

Instituto de Biología Celular

2D 3D TSV

10467133

Structural basis for selective inhibition of Src family kinases by PP1.

Chem Biol 6: 671-8 (1999)

Princeton University

2D 3D TSV

10465561

Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives.

Bioorg Med Chem Lett 9: 2279-82 (1999)

Purdue University

2D 3D TSV

10465559

Significant compensatory role of position Y-2 conferring high affinity to non-phosphorylated inhibitors of Grb2-SH2 domain.

Bioorg Med Chem Lett 9: 2267-72 (1999)

National Cancer Institute-Bethesda

2D 3D TSV

10465557

Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1' substituents.

Bioorg Med Chem Lett 9: 2259-62 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10465552

3-Alkyl-(5,5'-diphenyl)imidazolidineiones as new cannabinoid receptor ligands.

Bioorg Med Chem Lett 9: 2233-6 (1999)

Universit£ Catholiqu£ de Louvain

2D 3D TSV

10465550

Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK).

Bioorg Med Chem Lett 9: 2223-8 (1999)

Novartis Institute for BioMedical Research

2D 3D TSV

10465549

Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety.

Bioorg Med Chem Lett 9: 2217-22 (1999)

Parke-Davis Pharmaceutical Research

2D 3D TSV

10465547

SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor.

Bioorg Med Chem Lett 9: 2207-12 (1999)

Merck Frosst Centre for Therapeutic Research

2D 3D TSV

10465539

Synthesis of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists.

Bioorg Med Chem Lett 9: 2173-6 (1999)

F. Hoffmann-La Roche Inc

2D 3D TSV

10465538

Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.

Bioorg Med Chem Lett 9: 2167-72 (1999)

Uppsala University

2D 3D TSV

10465535

Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers.

Bioorg Med Chem Lett 9: 2151-6 (1999)

Warner-Lambert Company

2D 3D TSV

10465529

Novel conformationally restricted tetracyclic analogs of delta8-tetrahydrocannabinol.

Bioorg Med Chem Lett 9: 2119-24 (1999)

University of Connecticut

2D 3D TSV

10465404

Synthesis and in vitro evaluation of novel 2,6,9-trisubstituted purines acting as cyclin-dependent kinase inhibitors.

Bioorg Med Chem 7: 1281-93 (1999)

Institut Curie

2D 3D TSV

10464027

Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.

J Med Chem 42: 3412-20 (1999)

University of Oregon

2D 3D TSV

118

10464022

Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase.

J Med Chem 42: 3356-68 (1999)

Merck Research Laboratories

2D 3D TSV

10464021

N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.

J Med Chem 42: 3342-55 (1999)

Knoll Pharmaceuticals

2D 3D TSV

10464020

Thiazolothiazepine inhibitors of HIV-1 integrase.

J Med Chem 42: 3334-41 (1999)

National Cancer Institute-Bethesda

2D 3D TSV

10464018

Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.

J Med Chem 42: 3315-23 (1999)

University of Kansas

2D 3D TSV

10464016

Synthesis and properties of 3-(2-hydroxyethyl)-3-n-pentyldiazirine, a photoactivable general anesthetic.

J Med Chem 42: 3300-7 (1999)

Massachusetts General Hospital

2D 3D TSV

10464012

New 4-point pharmacophore method for molecular similarity and diversity applications: overview of the method and applications, including a novel approach to the design of combinatorial libraries containing privileged substructures.

J Med Chem 42: 3251-64 (1999)

Rh£ne-Poulenc Rorer

2D 3D TSV

10464010

Synthesis, in vitro pharmacology, and molecular modeling of very potent tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease.

J Med Chem 42: 3227-42 (1999)

Universitat de Barcelona

2D 3D TSV

10464008

Lead generation using pharmacophore mapping and three-dimensional database searching: application to muscarinic M(3) receptor antagonists.

J Med Chem 42: 3210-6 (1999)

Astra Charnwood

2D 3D TSV

10464006

PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3-d]thiophenes.

J Med Chem 42: 3199-202 (1999)

Wyeth-Ayerst Research

2D 3D TSV

10455277

Ligand efficacy and potency at recombinant human MT2 melatonin receptors: evidence for agonist activity of some mt1-antagonists.

Br J Pharmacol 127: 1288-94 (1999)

Universit&agrove; degli Studi di Milano

2D 3D TSV

10455251

RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.

Br J Pharmacol 127: 1075-82 (1999)

Roche Bioscience

2D 3D TSV

10454469

Native gamma-aminobutyric acid type A receptors from rat hippocampus, containing both alpha 1 and alpha 5 subunits, exhibit a single benzodiazepine binding site with alpha 5 pharmacological properties.

J Pharmacol Exp Ther 290: 989-97 (1999)

Universidad de Sevilla

2D 3D TSV

10450992

Tetrapeptide derived inhibitors of complexation of a class II MHC: fully unnatural ligands.

Bioorg Med Chem Lett 9: 2115-8 (1999)

Merck Research Laboratories

2D 3D TSV

10450991

Tetrapeptide derived inhibitors of complexation of a class II MHC: the peptide backbone is not inviolate.

Bioorg Med Chem Lett 9: 2109-14 (1999)

Merck Research Laboratories

2D 3D TSV

10450990

1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase.

Bioorg Med Chem Lett 9: 2105-8 (1999)

Cardiff University

2D 3D TSV

10450988

Synthesis and evaluation of hydroxyproline-derived isoprenyltransferase inhibitors.

Bioorg Med Chem Lett 9: 2095-100 (1999)

Eisai Research Institute

2D 3D TSV

10450987

Potent immunosuppressive C32-O-arylethyl ether derivatives of ascomycin with reduced toxicity.

Bioorg Med Chem Lett 9: 2089-94 (1999)

Merck Research Laboratories

2D 3D TSV

10450986

C32-O-phenalkyl ether derivatives of the immunosuppressant ascomycin: a tether length study.

Bioorg Med Chem Lett 9: 2085-8 (1999)

Merck Research Laboratories

2D 3D TSV

10450984

Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.

Bioorg Med Chem Lett 9: 2073-8 (1999)

Schering-Plough Research Institute

2D 3D TSV

10450981

Novel benzopyrano[3,4-c]pyrrole derivatives as potent and selective dopamine D3 receptor antagonist.

Bioorg Med Chem Lett 9: 2059-64 (1999)

Centre de Recherches de Croissy

2D 3D TSV

10450980

Design and synthesis of beta-carboxamido phosphonates as potent inhibitors of imidazole glycerol phosphate dehydratase.

Bioorg Med Chem Lett 9: 2053-8 (1999)

Monsanto Company

2D 3D TSV

10450979

Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents.

Bioorg Med Chem Lett 9: 2049-52 (1999)

University of Cambridge

2D 3D TSV

10450977

Polyunsaturated fatty acid anilides as inhibitors of acyl-coA: cholesterol acyltransferase (ACAT).

Bioorg Med Chem Lett 9: 2039-42 (1999)

Azwell Inc.

2D 3D TSV

10450976

Stereoselective synthesis of a new muscarinic M3 receptor antagonist, J-104129.

Bioorg Med Chem Lett 9: 2037-8 (1999)

Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories

2D 3D TSV

10450973

4-hydroxy-5,6-dihydro-2H-pyran-2-ones.3. Bicyclic and hetero-aromatic ring systems as 3-position scaffolds to bind to S1' and S2' of the HIV-1 protease enzyme.

Bioorg Med Chem Lett 9: 2019-24 (1999)

Warner-Lambert Company

2D 3D TSV

10450972

Design and synthesis of a novel synthetic NAPAP-penta-saccharide conjugate displaying a dual antithrombotic action.

Bioorg Med Chem Lett 9: 2013-8 (1999)

Gorlaeus Laboratories

2D 3D TSV

10450969

The synthesis and evaluation of 6-alkylidene-2'beta-substituted penam sulfones as beta-lactamase inhibitors.

Bioorg Med Chem Lett 9: 1997-2002 (1999)

Southern Methodist University

2D 3D TSV

10450968

Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.

Bioorg Med Chem Lett 9: 1991-6 (1999)

Merck Research Laboratories

2D 3D TSV

10450967

The design and synthesis of inhibitors of adenosine 5'-monophosphate deaminase.

Bioorg Med Chem Lett 9: 1985-90 (1999)

AgrEvo UK Limited

2D 3D TSV

10450966

Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist.

Bioorg Med Chem Lett 9: 1979-84 (1999)

Fujisawa Pharmaceutical Co., Ltd

2D 3D TSV

10450965

Structure-based design of a non-peptidic antagonist of the SH2 domain of GRB2.

Bioorg Med Chem Lett 9: 1973-8 (1999)

Novartis Pharmaceuticals

2D 3D TSV

10450964

2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands.

Bioorg Med Chem Lett 9: 1969-72 (1999)

Universität Erlangen - Nürnberg

2D 3D TSV

10450962

Structure-based design and synthesis of novel thrombin inhibitors based on phosphinic peptide mimetics.

Bioorg Med Chem Lett 9: 1957-62 (1999)

University of Illinois at Chicago

2D 3D TSV

10450960

Isolation and structure of SCH 351633: a novel hepatitis C virus (HCV) NS3 protease inhibitor from the fungus Penicillium griseofulvum.

Bioorg Med Chem Lett 9: 1949-52 (1999)

Schering-Plough Research Institute

2D 3D TSV

10450955

The design and synthesis of ALS inhibitors from pharmacophore models.

Bioorg Med Chem Lett 9: 1927-32 (1999)

Nankai University

2D 3D TSV

10450951

Design and synthesis of diaminopyrrolidinone inhibitors of human osteoclast cathepsin K.

Bioorg Med Chem Lett 9: 1907-10 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10450950

Design of benzoic acid inhibitors of influenza neuraminidase containing a cyclic substitution for the N-acetyl grouping.

Bioorg Med Chem Lett 9: 1901-6 (1999)

University of Alabama at Birmingham

2D 3D TSV

10450949

Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling.

Bioorg Med Chem Lett 9: 1895-900 (1999)

Wyeth-Ayerst Research

2D 3D TSV

10447965

Synthesis and biological activity of the superestrogen (E)-17-oximino-3-O-sulfamoyl-1,3,5(10)-estratriene: x-ray crystal structure of (E)-17-oximino-3-hydroxy-1,3,5(10)-estratriene.

J Med Chem 42: 3188-92 (1999)

University of Bath

2D 3D TSV

10447960

Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.

J Med Chem 42: 3154-62 (1999)

Universidad de Valencia

2D 3D TSV

10447959

N(omega)-Nitroarginine-containing dipeptide amides. Potent and highly selective inhibitors of neuronal nitric oxide synthase.

J Med Chem 42: 3147-53 (1999)

Northwestern University

2D 3D TSV

10447957

Carboxylic acid analogues of tamoxifen: (Z)-2-[p-(1, 2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine. Estrogen receptor affinity and estrogen antagonist effects in MCF-7 cells.

J Med Chem 42: 3126-33 (1999)

University of Georgia

2D 3D TSV

10447955

Potent bivalent thrombin inhibitors: replacement of the scissile peptide bond at P(1)-P(1)' with arginyl ketomethylene isosteres.

J Med Chem 42: 3109-15 (1999)

National Research Council Canada

2D 3D TSV

10447952

Lipophilic 4-isoxazolyl-1,4-dihydropyridines: synthesis and structure-activity relationships.

J Med Chem 42: 3087-93 (1999)

State University of New York

2D 3D TSV

10447950

Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions.

J Med Chem 42: 3066-74 (1999)

Targacept Inc

2D 3D TSV

10447949

Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.

J Med Chem 42: 3055-65 (1999)

National Institute of Diabetes

2D 3D TSV

10447947

N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists.

J Med Chem 42: 3033-40 (1999)

Technische Universität München

2D 3D TSV

10447946

Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist.

J Med Chem 42: 3026-32 (1999)

BASF AG

2D 3D TSV

10447942

A novel acetylated analogue of dynorphin A-(1-11) amide as a kappa-opioid receptor antagonist.

J Med Chem 42: 3011-3 (1999)

TBA

2D 3D TSV

10445051

Thiazole derivatives as inhibitors of purified bovine liver mitochondrial monoamine oxidase-B: structure-activity relationships and theoretical study.

J Enzym Inhib 14: 307-21 (1999)

University of Catania

2D 3D TSV

10433861

Somatostatin and its receptor family.

Front Neuroendocrinol 20: 157-98 (1999)

Royal Victoria Hospital

2D 3D TSV

10425145

Activity-guided isolation of triterpenoid acyl CoA cholesteryl acyl transferase (ACAT) inhibitors from Ilex kudincha.

J Nat Prod 62: 1061-4 (1999)

Kayaku Co. Ltd.

2D 3D TSV

10425142

New guaianolides and xanthine oxidase inhibitory flavonols from ajania fruticulosa

J Nat Prod 62: 1053-5 (1999)

Nanjing University

2D 3D TSV

10425125

Harbinatic acid, a novel and potent DNA polymerase beta inhibitor from Hardwickia binata.

J Nat Prod 62: 1000-2 (1999)

University of Virginia

2D 3D TSV

10425111

Importance of the aromatic residue at position 6 of [Nle(10)]neurokinin A(4-10) for binding to the NK-2 receptor and receptor activation.

J Med Chem 42: 3004-7 (1999)

Creighton University School of Medicine

2D 3D TSV

10425110

Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives.

J Med Chem 42: 3001-3 (1999)

Mitsui Pharmaceuticals Inc.

2D 3D TSV

10425109

4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.

J Med Chem 42: 2993-3000 (1999)

CoCensys Inc

2D 3D TSV

10425106

4-Heterocyclohexanone-based inhibitors of the serine protease plasmin.

J Med Chem 42: 2969-76 (1999)

Brown University

2D 3D TSV

10425105

Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.

J Med Chem 42: 2961-8 (1999)

University of Camerino

2D 3D TSV

10425100

Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.

J Med Chem 42: 2909-19 (1999)

Universität Hamburg

2D 3D TSV

10425096

2,3-Dihydro-2-oxo-1H-benzimidazole-1-carboxamides with selective affinity for the 5-HT(4) receptor: synthesis and structure-affinity and structure-activity relationships of a new series of partial agonist and antagonist derivatives.

J Med Chem 42: 2870-80 (1999)

FAES, S.A.

2D 3D TSV

10425095

Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation.

J Med Chem 42: 2862-9 (1999)

University of Minnesota

2D 3D TSV

10425088

Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical antipsychotics.

J Med Chem 42: 2774-97 (1999)

Universidad de Santiago

2D 3D TSV

101

10425087

Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.

J Med Chem 42: 2760-73 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

110

10425086

Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.

J Med Chem 42: 2752-9 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10425084

(R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides are orally active inhibitors of pyruvate dehydrogenase kinase.

J Med Chem 42: 2741-6 (1999)

Novartis Institute for Biomedical Research

2D 3D TSV

10425083

2-(2-Phenylcyclopropyl)imidazolines: reversed enantioselective interaction at I(1) and I(2) imidazoline receptors.

J Med Chem 42: 2737-40 (1999)

Universit£ di Camerino

2D 3D TSV

10425082

Pharmacotherapies for treatment of cocaine abuse: preclinical aspects.

J Med Chem 42: 2721-36 (1999)

Research Triangle Institute

2D 3D TSV

10421757

Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.

Chem Biol 6: 519-29 (1999)

Institute of Genetics and Molecular and Cellular Biology (IGBMC)

2D 3D TSV

10421658

Transport of monoglucuronosyl and bisglucuronosyl bilirubin by recombinant human and rat multidrug resistance protein 2.

Hepatology 30: 485-90 (1999)

Deutsches Krebsforschungszentrum

2D 3D TSV

10417407

Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin.

Acta Crystallogr D Biol Crystallogr 55: 1395-404 (1999)

Berlex

2D 3D TSV

10417314

Characterization of the high-affinity monocarboxylate transporter MCT2 in Xenopus laevis oocytes.

Biochem J 341: 529-35 (1999)

Physiologisch-chemisches Institut der Eberhard-Karls-Universit£t T£bingen

2D 3D TSV

10411602

Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.

J Pharmacol Exp Ther 290: 854-62 (1999)

Eli Lilly and Company

2D 3D TSV

10411589

Comparison of the pharmacological properties of cloned rat, human, and bovine norepinephrine transporters.

J Pharmacol Exp Ther 290: 761-7 (1999)

The University of Queensland

2D 3D TSV

10411588

Proteinase-activated receptor 2 (PAR(2)): development of a ligand-binding assay correlating with activation of PAR(2) by PAR(1)- and PAR(2)-derived peptide ligands.

J Pharmacol Exp Ther 290: 753-60 (1999)

The University of Calgary

2D 3D TSV

10411577

The interaction and transport of beta-lactam antibiotics with the cloned rat renal organic anion transporter 1.

J Pharmacol Exp Ther 290: 672-7 (1999)

Kyorin University

2D 3D TSV

10411562

Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles.

J Pharmacol Exp Ther 290: 551-60 (1999)

Merck Frosst Centre for Therapeutic Research

2D 3D TSV

10411492

(2R,1'S,2'R,3'S)-2-(2'-Carboxy-3'-phenylcyclopropyl)glycine (PCCG-13), the first potent and selective competitive antagonist of phospholipase D-coupled metabotropic glutamate receptors: asymmetric synthesis and preliminary biological properties.

J Med Chem 42: 2716-20 (1999)

Università di Perugia

2D 3D TSV

10411491

1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.

J Med Chem 42: 2706-15 (1999)

Merck Sharp and Dohme Research Laboratories

2D 3D TSV

10411488

2,7-Disubstituted amidofluorenone derivatives as inhibitors of human telomerase.

J Med Chem 42: 2679-84 (1999)

The Institute of Cancer Research

2D 3D TSV

10411485

Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.

J Med Chem 42: 2651-61 (1999)

Schering-Plough Research Institute

2D 3D TSV

10411484

Carbonic anhydrase inhibitors. Synthesis of water-soluble, topically effective, intraocular pressure-lowering aromatic/heterocyclic sulfonamides containing cationic or anionic moieties: is the tail more important than the ring?

J Med Chem 42: 2641-50 (1999)

Universit£ degli Studi

2D 3D TSV

176

10411483

alpha-Functionalized phosphonylphosphinates: synthesis and evaluation as transcarbamoylase inhibitors.

J Med Chem 42: 2633-40 (1999)

Universit£tstrasse 16

2D 3D TSV

10411482

1,3-Disubstituted benzazepines as novel, potent, selective neuropeptide Y Y1 receptor antagonists.

J Med Chem 42: 2621-32 (1999)

Shionogi & Company, Ltd.

2D 3D TSV

10411481

Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study.

J Med Chem 42: 2610-20 (1999)

CEA

2D 3D TSV

144

10411478

Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives.

J Med Chem 42: 2582-7 (1999)

BIAL

2D 3D TSV

10411472

Synthesis and serotonergic activity of substituted 2, N-benzylcarboxamido-5-(2-ethyl-1-dioxoimidazolidinyl)-N, N-dimethyltryptamine derivatives: novel antagonists for the vascular 5-HT(1B)-like receptor.

J Med Chem 42: 2504-26 (1999)

Monash University (Parkville Campus)

2D 3D TSV

10411471

Evaluation of PMF scoring in docking weak ligands to the FK506 binding protein.

J Med Chem 42: 2498-503 (1999)

Abbott Laboratories

2D 3D TSV

10406658

Analogs of 4-(3-bromo-8-methyl-10-methoxy-6,11-dihydro-5H-benzo[5,6]-cyclo hepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N-oxide as inhibitors of farnesyl protein transferase.

Bioorg Med Chem Lett 9: 1875-80 (1999)

Schering-Plough Research Institute

2D 3D TSV

10406657

Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.

Bioorg Med Chem Lett 9: 1869-74 (1999)

Merck Research Laboratories

2D 3D TSV

10406650

Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity.

Bioorg Med Chem Lett 9: 1831-6 (1999)

Georgetown University Medical Center

2D 3D TSV

10406649

From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.

Bioorg Med Chem Lett 9: 1825-30 (1999)

The James Black Foundation

2D 3D TSV

10406647

Multiple parallel synthesis of N,N-dialkyldipeptidylamines as N-type calcium channel blockers.

Bioorg Med Chem Lett 9: 1813-8 (1999)

Warner-Lambert Company

2D 3D TSV

10406646

Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.

Bioorg Med Chem Lett 9: 1807-12 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10406645

Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics.

Bioorg Med Chem Lett 9: 1801-6 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10406642

Synthesis and preliminary biological evaluation of new alpha-amino amide anticonvulsants incorporating a dextromethorphan moiety.

Bioorg Med Chem Lett 9: 1783-8 (1999)

Pharmacia & Upjohn

2D 3D TSV

10406640

The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.

Bioorg Med Chem Lett 9: 1773-8 (1999)

Merck Frosst Centre for Therapeutic Research

2D 3D TSV

10406637

Synthesis and identification of conformationally constrained selective MMP inhibitors.

Bioorg Med Chem Lett 9: 1757-60 (1999)

Searle Discovery Research

2D 3D TSV

10406636

Synthesis and evaluation of 1,4,5,6-tetrahydropyridazine derivatives as influenza neuraminidase inhibitors.

Bioorg Med Chem Lett 9: 1751-6 (1999)

Gilead Sciences Inc

2D 3D TSV

10406633

5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-yl carbonyl)-2-pyridinyl]benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists.

Bioorg Med Chem Lett 9: 1737-40 (1999)

Wyeth-Ayerst Research

2D 3D TSV

10406632

4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists.

Bioorg Med Chem Lett 9: 1733-6 (1999)

Wyeth-Ayerst Research

2D 3D TSV

10397508

1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties.

Bioorg Med Chem Lett 9: 1721-6 (1999)

Georgetown University Medical Center

2D 3D TSV

10397507

2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors.

Bioorg Med Chem Lett 9: 1715-20 (1999)

Merck Frosst Centre for Therapeutic Research

2D 3D TSV

10397504

Synthesis and evaluation of 1-position-modified inositol 1,4,5-trisphosphate analogs.

Bioorg Med Chem Lett 9: 1697-702 (1999)

The University of Tokyo

2D 3D TSV

10397503

Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors.

Bioorg Med Chem Lett 9: 1691-6 (1999)

Universit£ de Montr£al

2D 3D TSV

10397502

Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.

Bioorg Med Chem Lett 9: 1687-90 (1999)

Stanford University

2D 3D TSV

10397500

Design and synthesis of 2-[4-[4-(m-(ethylsulfonamido)-phenyl) piperazin-1-yl]butyl]-1,3-dioxoperhydropyrrolo[1,2-c]imidazole (EF-7412) using neural networks. A selective derivative with mixed 5-HT1A/D2 antagonist properties.

Bioorg Med Chem Lett 9: 1679-82 (1999)

Universidad Complutense

2D 3D TSV

10397495

Thrombin inhibitors based on [5,5] trans-fused indane lactams.

Bioorg Med Chem Lett 9: 1657-62 (1999)

Glaxo Wellcome Research and Development

2D 3D TSV

10397493

Derivation of a possible transition-state for the reaction catalysed by the enzyme estrone Sulfatase (ES).

Bioorg Med Chem Lett 9: 1645-50 (1999)

Kingston University

2D 3D TSV

10395524

A new tyrosine kinase inhibitor from the marine brown alga Stypopodium zonale.

J Nat Prod 62: 927-30 (1999)

Technical University of Braunschweig

2D 3D TSV

10395519

Interference of linoleic acid fraction in some receptor binding assays.

J Nat Prod 62: 912-4 (1999)

Leiden University

2D 3D TSV

10395489

4,5-Dihydro-1,2,4-triazolo[1,5-a]quinoxalin-4-ones: excitatory amino acid antagonists with combined glycine/NMDA and AMPA receptor affinity.

J Med Chem 42: 2478-84 (1999)

Universita' di Firenze

2D 3D TSV

10395488

Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(arylalkynyl)-4-benzylpiperidines.

J Med Chem 42: 2469-77 (1999)

CoCensys Inc

2D 3D TSV

114

10395486

Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase inhibitors and antitumor agents: synthesis and biological activities of 2,4-diamino-5-methyl-6-[(monosubstituted anilino)methyl] pyrido[2,3-d]pyrimidines.

J Med Chem 42: 2447-55 (1999)

Duquesne University

2D 3D TSV

10395483

Structure-activity relationships for a class of inhibitors of purine nucleoside phosphorylase.

J Med Chem 42: 2422-31 (1999)

University of Michigan

2D 3D TSV

10395482

Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.

J Med Chem 42: 2409-21 (1999)

Merck Research Laboratories

2D 3D TSV

10395480

Apstatin analogue inhibitors of aminopeptidase P, a bradykinin-degrading enzyme.

J Med Chem 42: 2394-402 (1999)

Pharmacia and Upjohn, Inc.

2D 3D TSV

103

10395478

Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor.

J Med Chem 42: 2373-82 (1999)

University of Auckland

2D 3D TSV

126

10395476

Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic.

J Med Chem 42: 2358-63 (1999)

Novartis Pharma Inc

2D 3D TSV

10395475

Pharmacophore development for corticotropin-releasing hormone: new insights into inhibitor activity.

J Med Chem 42: 2351-7 (1999)

The University of Wollongong

2D 3D TSV

10395474

Molecular modeling and synthesis of inhibitors of herpes simplex virus type 1 uracil-DNA glycosylase.

J Med Chem 42: 2344-50 (1999)

University of Massachusetts Medical Center

2D 3D TSV

10395473

Potent inhibition of influenza sialidase by a benzoic acid containing a 2-pyrrolidinone substituent.

J Med Chem 42: 2332-43 (1999)

University of Alabama at Birmingham

2D 3D TSV

10387041

Molecular recognition of macrocyclic peptidomimetic inhibitors by HIV-1 protease.

Biochemistry 38: 7978-88 (1999)

University of Queensland

2D 3D TSV

10386947

Structure-activity relationship for a series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles: potent subtype-selective inhibitors of N-methyl-D-aspartate (NMDA) receptors.

Bioorg Med Chem Lett 9: 1619-24 (1999)

University of Oregon

2D 3D TSV

10386946

Design of scytalone dehydratase inhibitors as rice blast fungicides: derivatives of norephedrine.

Bioorg Med Chem Lett 9: 1613-8 (1999)

FMC Stine Research Center

2D 3D TSV

10386945

Design of scytalone dehydratase inhibitors as rice blast fungicides: (N-phenoxypropyl)-carboxamides.

Bioorg Med Chem Lett 9: 1607-12 (1999)

FMC Stine Research Center

2D 3D TSV

10386944

N-substituted 4-(5-indolyl)benzoic acids. Synthesis and evaluation of steroid 5alpha-reductase type I and II inhibitory activity.

Bioorg Med Chem Lett 9: 1601-6 (1999)

Universität des Saarlandes

2D 3D TSV

10386942

Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.

Bioorg Med Chem Lett 9: 1593-8 (1999)

Institute

2D 3D TSV

10386940

Novel derivatives of 3-(dipropylamino)chroman. Interactions with 5-HT1A and D2A receptors.

Bioorg Med Chem Lett 9: 1583-6 (1999)

Uppsala University

2D 3D TSV

10386938

Structure-activity relationships of substituted 5H-thiazolo[3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists.

Bioorg Med Chem Lett 9: 1573-6 (1999)

F. Hoffmann-La Roche Inc

2D 3D TSV

10386934

Dual-acting agents with alpha1-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory activities. Synthesis and evaluation of arylpiperazine derivatives.

Bioorg Med Chem Lett 9: 1553-8 (1999)

Zeria Pharmaceutical Co., Ltd.

2D 3D TSV

10386932

Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.

Bioorg Med Chem Lett 9: 1541-6 (1999)

Eisai Research Institute

2D 3D TSV

10386929

The sulfonimidamide as a novel transition state analog for aspartic acid and metallo proteases.

Bioorg Med Chem Lett 9: 1527-32 (1999)

The University of Kansas

2D 3D TSV

10386926

Design of the first highly potent and selective aminopeptidase N (EC 3.4.11.2) inhibitor.

Bioorg Med Chem Lett 9: 1511-6 (1999)

University of Paris

2D 3D TSV

10386923

Synthesis and evaluation of glucocerebrosidase inhibitory activity of anhydro deoxyinositols from (+)-epi- and (-)-vibo-quercitols.

Bioorg Med Chem Lett 9: 1493-8 (1999)

Keio University

2D 3D TSV

10386921

Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl,5-methylphenyl thio) moiety: antiviral activities and pharmacokinetic properties.

Bioorg Med Chem Lett 9: 1481-6 (1999)

Warner-Lambert Company

2D 3D TSV

10385678

Selective substrates for non-neuronal monoamine transporters.

Mol Pharmacol 56: 1-10 (1999)

University of Heidelberg

2D 3D TSV

10379421

Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding.

Cell Mol Neurobiol 19: 467-89 (1999)

TBA

2D 3D TSV

134

10377455

Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis.

Proc Natl Acad Sci U S A 96: 7563-8 (1999)

St. Bartholomew's and the Royal London School of Medicine and Dentistry

2D 3D TSV

121

10377236

2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines: novel selective beta3-adrenoceptor agonists.

J Med Chem 42: 2287-94 (1999)

University of Tennessee

2D 3D TSV

10377235

Potent inhibition of steroid sulfatase activity by 3-O-sulfamate 17alpha-benzyl(or 4'-tert-butylbenzyl)estra-1,3,5(10)-trienes: combination of two substituents at positions C3 and c17alpha of estradiol.

J Med Chem 42: 2280-6 (1999)

Laval University

2D 3D TSV

10377234

Synthesis of classical and a nonclassical 2-amino-4-oxo-6-methyl-5-substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitors of thymidylate synthase.

J Med Chem 42: 2272-9 (1999)

Duquesne University

2D 3D TSV

10377231

Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.

J Med Chem 42: 2251-9 (1999)

CEA

2D 3D TSV

10377229

New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.

J Med Chem 42: 2235-44 (1999)

University of Göteborg

2D 3D TSV

107

10377228

Novel and potent 6-chloro-3-pyridinyl ligands for the alpha4beta2 neuronal nicotinic acetylcholine receptor.

J Med Chem 42: 2227-34 (1999)

University of California

2D 3D TSV

10377223

Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.

J Med Chem 42: 2180-90 (1999)

Merck Research Laboratories

2D 3D TSV

10377221

Butenolide endothelin antagonists with improved aqueous solubility.

J Med Chem 42: 2162-8 (1999)

Warner-Lambert Company

2D 3D TSV

10377218

Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.

J Med Chem 42: 2125-35 (1999)

Schering-Plough Research Institute

2D 3D TSV

10377217

Phthalein derivatives as a new tool for selectivity in thymidylate synthase inhibition.

J Med Chem 42: 2112-24 (1999)

Università di Modena e Reggio Emilia

2D 3D TSV

10377216

A peptide agonist acts by occupation of a monomeric G protein-coupled receptor: dual sites of covalent attachment to domains near TM1 and TM7 of the same molecule make biologically significant domain-swapped dimerization unlikely.

J Med Chem 42: 2105-11 (1999)

Mayo Clinic and Foundation

2D 3D TSV

10377215

Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.

J Med Chem 42: 2087-104 (1999)

Merck Sharp & Dohme Research Laboratories

2D 3D TSV

104

10377214

Structure-antiviral activity relationship in the series of pyrimidine and purine N-[2-(2-phosphonomethoxy)ethyl] nucleotide analogues. 1. Derivatives substituted at the carbon atoms of the base.

J Med Chem 42: 2064-86 (1999)

Academy of Sciences of the Czech Republic

2D 3D TSV

290

10375538

Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors.

Chem Biol 6: 361-75 (1999)

University of California Berkeley

2D 3D TSV

10374926

Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans.

Life Sci 64: 2011-20 (1999)

Hungarian Academy of Sciences

2D 3D TSV

10360758

Metallopeptide approach to the design of biologically active ligands: design of specific human neutrophil elastase inhibitors.

Bioorg Med Chem Lett 9: 1469-74 (1999)

Palatin Technologies Inc

2D 3D TSV

10360757

The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.

Bioorg Med Chem Lett 9: 1463-8 (1999)

Cardiff University

2D 3D TSV

10360755

P1, P2'-linked macrocyclic amine derivatives as matrix metalloproteinase inhibitors.

Bioorg Med Chem Lett 9: 1453-8 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10360754

Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases.

Bioorg Med Chem Lett 9: 1447-52 (1999)

Tartu University

2D 3D TSV

10360750

Uncarinic acids: phospholipase Cgamma1 inhibitors from hooks of Uncaria rhynchophylla.

Bioorg Med Chem Lett 9: 1429-32 (1999)

Seoul National University

2D 3D TSV

10360749

Heterocycle-peptide hybrid compounds. Aminotriazole-containing agonists of the thrombin receptor (PAR-1).

Bioorg Med Chem Lett 9: 1423-8 (1999)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10360746

Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands.

Bioorg Med Chem Lett 9: 1409-14 (1999)

Institut de Recherches Servier

2D 3D TSV

10360745

Piperidine-renin inhibitors compounds with improved physicochemical properties.

Bioorg Med Chem Lett 9: 1403-8 (1999)

F. Hoffmann-La Roche Inc

2D 3D TSV

10360744

Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.

Bioorg Med Chem Lett 9: 1397-402 (1999)

F. Hoffmann-La Roche Inc

2D 3D TSV

10360741

Efficient inhibition of muscle and liver glycogen phosphorylases by a new glucopyranosylidene-spiro-thiohydantoin.

Bioorg Med Chem Lett 9: 1385-90 (1999)

Lajos Kossuth University

2D 3D TSV

10360740

N-substituted-3-arylpyrrolidines: potent and selective ligands at serotonin 1A receptor.

Bioorg Med Chem Lett 9: 1379-84 (1999)

POSTECH

2D 3D TSV

10360739

Acyl-CoA: cholesterol acyltransferase inhibitory activity of ginseng sapogenins, produced from the ginseng saponins.

Bioorg Med Chem Lett 9: 1375-8 (1999)

Korea Research Institute of Bioscience and Biotechnology

2D 3D TSV

10360738

Synthesis and protein kinase C binding activity of benzolactam-V7.

Bioorg Med Chem Lett 9: 1371-4 (1999)

Institute of Organic Chemistry

2D 3D TSV

10360736

S1319: a novel beta2-andrenoceptor agonist from a marine sponge Dysidea sp.

Bioorg Med Chem Lett 9: 1361-4 (1999)

Kirin Brewery Co., Ltd

2D 3D TSV

10360732

trans-2,6-,3,6- and 4,6-diaza-5,6,6a,7,8,12b-hexahydro-benzo[c]phenanthrene-10,11- diols as dopamine agonists.

Bioorg Med Chem Lett 9: 1341-6 (1999)

Abbott Laboratories

2D 3D TSV

10354414

Synthesis and pharmacology of the baclofen homologues 5-amino-4-(4-chlorophenyl)pentanoic acid and the R- and S-enantiomers of 5-amino-3-(4-chlorophenyl)pentanoic acid.

J Med Chem 42: 2053-9 (1999)

The Royal Danish School of Pharmacy

2D 3D TSV

10354412

Simplified pepstatins: synthesis and evaluation of N-terminally modified analogues.

J Med Chem 42: 2041-5 (1999)

Institute of Pharmaceutical Chemistry and Institute of Pharmaceutical Technology

2D 3D TSV

10354409

New generation dopaminergic agents. 6. Structure-activity relationship studies of a series of 4-(aminoethoxy)indole and 4-(aminoethoxy)indolone derivatives based on the newly discovered 3-hydroxyphenoxyethylamine D2 template.

J Med Chem 42: 2007-20 (1999)

Wyeth-Ayerst Research Laboratories

2D 3D TSV

131

10354408

1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.

J Med Chem 42: 1999-2006 (1999)

Novo Nordisk A/S

2D 3D TSV

10354407

Synthesis, calcium mobilizing, and physicochemical properties of D-chiro-inositol 1,3,4,6-tetrakisphosphate, a novel and potent ligand at the D-myo-inositol 1,4,5-trisphosphate receptor.

J Med Chem 42: 1991-8 (1999)

University of Bath

2D 3D TSV

10354406

3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.

J Med Chem 42: 1982-90 (1999)

University of Kansas

2D 3D TSV

10354405

Unique analogues of anandamide: arachidonyl ethers and carbamates and norarachidonyl carbamates and ureas.

J Med Chem 42: 1975-81 (1999)

Organix Inc

2D 3D TSV

10354404

Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a.

J Med Chem 42: 1965-74 (1999)

University of Queensland

2D 3D TSV

10354399

Quantitative structure-activity relationship of human neutrophil collagenase (MMP-8) inhibitors using comparative molecular field analysis and X-ray structure analysis.

J Med Chem 42: 1908-20 (1999)

Hoechst Marion Roussel Inc

2D 3D TSV

10354398

Lamellarin alpha 20-sulfate, an inhibitor of HIV-1 integrase active against HIV-1 virus in cell culture.

J Med Chem 42: 1901-7 (1999)

Institute of Chemical Technology

2D 3D TSV

10354397

Isoxazolo-[3,4-d]-pyridazin-7-(6H)-one as a potential substrate for new aldose reductase inhibitors.

J Med Chem 42: 1894-900 (1999)

Dipartimento di Scienze Farmaceutiche

2D 3D TSV

10354396

1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.

J Med Chem 42: 1881-93 (1999)

Universit£ di Modena

2D 3D TSV

10354394

Highly potent cyclic disulfide antagonists of somatostatin.

J Med Chem 42: 1863-71 (1999)

Tulane University School of Medicine

2D 3D TSV

216

10353842

Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R).

Biochemistry 38: 7307-20 (1999)

National Institute of Diabetes and Digestive and Kidney Diseases

2D 3D TSV

147

10347254

Cloning and functional expression of the human histamine H3 receptor.

Mol Pharmacol 55: 1101-7 (1999)

R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

10346939

Synthesis of novel phenserine-based-selective inhibitors of butyrylcholinesterase for Alzheimer's disease.

J Med Chem 42: 1855-61 (1999)

National Institute on Aging Intramural Research Program

2D 3D TSV

10346937

Synthesis and evaluation of new sulfur-containing L-arginine-derived inhibitors of nitric oxide synthase.

J Med Chem 42: 1842-8 (1999)

Wake Forest University

2D 3D TSV

10346932

Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.

J Med Chem 42: 1803-15 (1999)

University of Auckland

2D 3D TSV

10346931

Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine.

J Med Chem 42: 1789-802 (1999)

Japan Energy Corporation

2D 3D TSV

10346928

Ligands for the tyrosine kinase p56lck SH2 domain: discovery of potent dipeptide derivatives with monocharged, nonhydrolyzable phosphate replacements.

J Med Chem 42: 1757-66 (1999)

Boehringer Ingelheim Pharmaceuticals Inc

2D 3D TSV

10346927

Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.

J Med Chem 42: 1749-56 (1999)

Berlex Biosciences

2D 3D TSV

114

10346925

Homology modeling of gelatinase catalytic domains and docking simulations of novel sulfonamide inhibitors.

J Med Chem 42: 1723-38 (1999)

Shionogi & Company, Ltd.

2D 3D TSV

10346920

4-[[2-(1-Methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride (SIB-1553A): a novel cognitive enhancer with selectivity for neuronal nicotinic acetylcholine receptors.

J Med Chem 42: 1684-6 (1999)

SIBIA Neurosciences Inc

2D 3D TSV

10340630

Venlafaxine: discrepancy between in vivo 5-HT and NE reuptake blockade and affinity for reuptake sites.

Synapse 32: 198-211 (1999)

McGill University

2D 3D TSV

10340624

4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.

Bioorg Med Chem Lett 9: 1335-40 (1999)

Ligand Pharmaceuticals Inc

2D 3D TSV

10340623

Synthesis of novel analogues of the delta opioid ligand SNC-80 using AlCl3-promoted aminolysis.

Bioorg Med Chem Lett 9: 1329-34 (1999)

Organon Laboratories Ltd

2D 3D TSV

10340622

Synthesis of novel analogues of the delta opioid ligand SNC-80 using REM resin.

Bioorg Med Chem Lett 9: 1323-8 (1999)

Organon Laboratories Ltd

2D 3D TSV

10340621

Optimisation of the P2 pharmacophore in a series of thrombin inhibitors: ion-dipole interactions with lysine 60G.

Bioorg Med Chem Lett 9: 1317-22 (1999)

Novartis Horsham Research Center

2D 3D TSV

10340620

Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.

Bioorg Med Chem Lett 9: 1311-6 (1999)

Merck Research Laboratories

2D 3D TSV

10340616

Synthesis and in vitro and in vivo evaluation of the 2-(6'methoxy-3',4'-dihydro-1'-naphtyl)-4H-3,1-benzoxazin-4- one as a new potent substrate inhibitor of human leukocyte elastase.

Bioorg Med Chem Lett 9: 1291-4 (1999)

Università degli Studi di L'Aquila

2D 3D TSV

10340615

4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.

Bioorg Med Chem Lett 9: 1285-90 (1999)

Merck Sharp and Dohme Research Laboratories

2D 3D TSV

10340614

Macrocyclic hydroxamate inhibitors of matrix metalloproteinases and TNF-alpha production.

Bioorg Med Chem Lett 9: 1279-84 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10340613

Inhibition of human telomerase by PNA-cationic peptide conjugates.

Bioorg Med Chem Lett 9: 1273-8 (1999)

University of Cambridge

2D 3D TSV

10340610

Isotope edited NMR studies of glycosidases: design and synthesis of a novel glycosidase inhibitor.

Bioorg Med Chem Lett 9: 1255-60 (1999)

Ohio State University

2D 3D TSV

10340609

L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.

Bioorg Med Chem Lett 9: 1251-4 (1999)

Merck Research Laboratories

2D 3D TSV

10340605

Synthesis and evaluation of geldanamycin-estradiol hybrids.

Bioorg Med Chem Lett 9: 1233-8 (1999)

Sloan-Kettering Institute for Cancer Research

2D 3D TSV

10340604

Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety.

Bioorg Med Chem Lett 9: 1227-32 (1999)

Research and Development

2D 3D TSV

10340602

Synthesis and biological activities of topoisomerase I inhibitors, 6-N-amino analogues of NB-506.

Bioorg Med Chem Lett 9: 1219-24 (1999)

Banyu Tsukuba Research Institute

2D 3D TSV

100

10336515

Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist.

J Pharmacol Exp Ther 289: 1262-70 (1999)

Banyu Pharmaceutical Co., Ltd.

2D 3D TSV

10336510

Pharmacological characterization of nicotine's interaction with cocaine and cocaine analogs.

J Pharmacol Exp Ther 289: 1229-36 (1999)

Virginia Commonwealth University

2D 3D TSV

10329466

Synthesis of the quinoline-linked triazolopyrimidine analogues and their interactions with the recombinant tobacco acetolactate synthase.

Biochem Biophys Res Commun 258: 797-801 (1999)

Seoul Women's University

2D 3D TSV

10328312

Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.

Bioorg Med Chem Lett 9: 1195-200 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10328310

Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.

Bioorg Med Chem Lett 9: 1185-8 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10328309

Structure-based design of diaminopyranosides as a novel inhibitor core unit of HIV proteases.

Bioorg Med Chem Lett 9: 1179-84 (1999)

Biomolecular Engineering Research Institute

2D 3D TSV

10328307

Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors.

Bioorg Med Chem Lett 9: 1171-4 (1999)

G.D. Searle-Monsanto

2D 3D TSV

10328306

Design and synthesis of sulfonyl-substituted 4,5-diarylthiazoles as selective cyclooxygenase-2 inhibitors.

Bioorg Med Chem Lett 9: 1167-70 (1999)

G.D. Searle-Monsanto

2D 3D TSV

10328300

Synthesis and biological activity of trans-2,3-dihydroraloxifene.

Bioorg Med Chem Lett 9: 1137-40 (1999)

Eli Lilly and Company

2D 3D TSV

10328297

Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers.

Bioorg Med Chem Lett 9: 1121-6 (1999)

Warner-Lambert Company

2D 3D TSV

10328293

The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.

Bioorg Med Chem Lett 9: 1103-8 (1999)

Novartis Horsham Research Centre

2D 3D TSV

10328291

Synthesis of caged peptides using caged lysine: application to the synthesis of caged AIP, a highly specific inhibitor of calmodulin-dependent protein kinase II.

Bioorg Med Chem Lett 9: 1093-6 (1999)

Osaka National Research Institute

2D 3D TSV

10328287

Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase.

Bioorg Med Chem Lett 9: 1069-74 (1999)

Abbott Laboratories

2D 3D TSV

10327430

Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes.

Neuropsychopharmacology 20: 612-27 (1999)

University of North Carolina

2D 3D TSV

10322128

Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3.

Chem Biol 6: 265-75 (1999)

Ligand Pharmaceuticals Inc

2D 3D TSV

10322126

Structure-based discovery and in-parallel optimization of novel competitive inhibitors of thymidylate synthase.

Chem Biol 6: 319-31 (1999)

Northwestern University

2D 3D TSV

10230641

Use of the Suzuki reaction for the synthesis of aryl-substituted heterocycles as corticotropin-releasing hormone (CRH) antagonists.

Bioorg Med Chem Lett 9: 1063-6 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10230640

4-Aryl-2-anilinopyrimidines as corticotropin-releasing hormone (CRH) antagonists.

Bioorg Med Chem Lett 9: 1057-62 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10230630

Thrombin inhibitors based on a propargylglycine template.

Bioorg Med Chem Lett 9: 1013-8 (1999)

Biotech Research Institute

2D 3D TSV

10230629

Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone.

Bioorg Med Chem Lett 9: 1009-12 (1999)

Ligand Pharmaceuticals Inc

2D 3D TSV

10230628

Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.

Bioorg Med Chem Lett 9: 1003-8 (1999)

Ligand Pharmaceuticals

2D 3D TSV

10230627

6-(1-Hydroxyalkyl))penam sulfone derivatives as inhibitors of class A and class C beta-lactamases II.

Bioorg Med Chem Lett 9: 997-1002 (1999)

Wyeth-Ayerst Research

2D 3D TSV

10230626

6-(1-Hydroxyalkyl)penam sulfone derivatives as inhibitors of class A and class C beta-lactamases I.

Bioorg Med Chem Lett 9: 991-6 (1999)

Wyeth-Ayerst Research

2D 3D TSV

10230624

N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase.

Bioorg Med Chem Lett 9: 979-84 (1999)

The R. W. Johnson Pharmaceutical Research Institute

2D 3D TSV

110

10230623

Synthesis of dihydroxanthone derivatives and evaluation of their inhibitory activity against acetylcholinesterase: unique structural analogs of tacrine based on the BCD-ring of arisugacin.

Bioorg Med Chem Lett 9: 973-8 (1999)

University of Minnesota

2D 3D TSV

10230622

Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.

Bioorg Med Chem Lett 9: 967-72 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10230616

Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols.

Bioorg Med Chem Lett 9: 943-8 (1999)

Searle Discovery Research

2D 3D TSV

10230615

Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: identification of alphavbeta3 antagonists lead compounds.

Bioorg Med Chem Lett 9: 937-42 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10230614

Adenosine receptor ligands with oxygenated N6-substituents.

Bioorg Med Chem Lett 9: 933-6 (1999)

Deakin University

2D 3D TSV

10230612

Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.

Bioorg Med Chem Lett 9: 925-30 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10230611

Terphenyl cyclooxygenase-2 (COX-2) inhibitors: optimization of the central ring and o-biphenyl analogs.

Bioorg Med Chem Lett 9: 919-24 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10230610

Synthesis and structure-activity relationship of potent bicyclic lactam thrombin inhibitors.

Bioorg Med Chem Lett 9: 913-8 (1999)

BioChem Therapeutic Inc.

2D 3D TSV

10229636

delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.

J Med Chem 42: 1673-9 (1999)

National Institute of Diabetes

2D 3D TSV

10229633

Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.

J Med Chem 42: 1648-60 (1999)

Pierre Fabre Research Center

2D 3D TSV

130

10229632

Cyclobutane quisqualic acid analogues as selective mGluR5a metabotropic glutamic acid receptor ligands.

J Med Chem 42: 1639-47 (1999)

University of Minnesota

2D 3D TSV

10229631

Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists.

J Med Chem 42: 1625-38 (1999)

National Institute of Diabetes

2D 3D TSV

10229627

Development of fluorine-18-labeled 5-HT1A antagonists.

J Med Chem 42: 1576-86 (1999)

National Institutes of Health

2D 3D TSV

10229626

Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.

J Med Chem 42: 1556-75 (1999)

Universit£ di Siena

2D 3D TSV

10229625

Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.

J Med Chem 42: 1546-55 (1999)

Parc Club Orsay Université

2D 3D TSV

10229624

Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel.

J Med Chem 42: 1537-45 (1999)

University of Alabama at Birmingham

2D 3D TSV

10229623

Synthesis of a series of stromelysin-selective thiadiazole urea matrix metalloproteinase inhibitors.

J Med Chem 42: 1525-36 (1999)

Pharmacia and Upjohn, Inc.

2D 3D TSV

10229620

Potent estrogenic agonists bearing dicarba-closo-dodecaborane as a hydrophobic pharmacophore.

J Med Chem 42: 1501-4 (1999)

University of Tokyo

2D 3D TSV

10229619

Emerging molecular approaches to pain therapy.

J Med Chem 42: 1481-500 (1999)

Abbott Laboratories

2D 3D TSV

10227113

Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro.

Schizophr Res 37: 107-22 (1999)

Eli Lilly and Company

2D 3D TSV

10224099

Structural elements of the gamma-aminobutyric acid type A receptor conferring subtype selectivity for benzodiazepine site ligands.

J Biol Chem 274: 13370-4 (1999)

Synthélabo

2D 3D TSV

10220855

A transfected cell model for the renal toxin transporter, rOCT2.

Toxicol Sci 47: 181-6 (1999)

University of Texas M. D. Anderson Cancer Center

2D 3D TSV

10220563

Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes.

Mol Pharmacol 55: 847-54 (1999)

Kyorin University

2D 3D TSV

10218828

Evaluation of short-tether bis-THA AChE inhibitors. A further test of the dual binding site hypothesis.

Bioorg Med Chem 7: 351-7 (1999)

Hong Kong University of Science and Technology

2D 3D TSV

10215699

Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands.

J Pharmacol Exp Ther 289: 1151-9 (1999)

Gliatech Inc

2D 3D TSV

10215672

Receptor binding, behavioral, and electrophysiological profiles of nonpeptide corticotropin-releasing factor subtype 1 receptor antagonists CRA1000 and CRA1001.

J Pharmacol Exp Ther 289: 926-35 (1999)

Taisho Pharmaceutical Co., Ltd

2D 3D TSV

10212133

5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a novel class of nonsteroidal progesterone receptor agonists: effect of A-ring modification.

J Med Chem 42: 1466-72 (1999)

Ligand Pharmaceuticals Inc

2D 3D TSV

10212129

Potent, low-molecular-weight non-peptide inhibitors of malarial aspartyl protease plasmepsin II.

J Med Chem 42: 1428-40 (1999)

University of California

2D 3D TSV

10212126

Chicoric acid analogues as HIV-1 integrase inhibitors.

J Med Chem 42: 1401-14 (1999)

National Cancer Institute-Bethesda

2D 3D TSV

10212125

N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.

J Med Chem 42: 1393-400 (1999)

Leiden/Amsterdam Center for Drug Research

2D 3D TSV

10212124

5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.

J Med Chem 42: 1384-92 (1999)

Leiden University

2D 3D TSV

10212123

Bound structures of novel P3-P1' beta-strand mimetic inhibitors of thrombin.

J Med Chem 42: 1376-83 (1999)

Michigan State University

2D 3D TSV

10212122

Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.

J Med Chem 42: 1367-75 (1999)

Molecumetics Ltd.

2D 3D TSV

10212120

Identification of highly selective inhibitors of collagenase-1 from combinatorial libraries of diketopiperazines.

J Med Chem 42: 1348-57 (1999)

Affymax Research Institute

2D 3D TSV

10212118

Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.

J Med Chem 42: 1333-40 (1999)

Yale University

2D 3D TSV

10206559

N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers.

Bioorg Med Chem Lett 9: 907-12 (1999)

Warner-Lambert Company

2D 3D TSV

10206558

Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.

Bioorg Med Chem Lett 9: 901-6 (1999)

Schering-Plough Research Institute

2D 3D TSV

10206557

Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals.

Bioorg Med Chem Lett 9: 895-900 (1999)

Corvas International Inc

2D 3D TSV

10206553

Combined NK1 and NK2 tachykinin receptor antagonists: synthesis and structure-activity relationships of novel oxazolidine analogues.

Bioorg Med Chem Lett 9: 875-80 (1999)

Sankyo Co., Ltd

2D 3D TSV

10206551

Nonpeptide glycoprotein IIB/IIIA inhibitors. 19. A new design paradigm employing linearly minimized, centrally constrained, exosite inhibitors.

Bioorg Med Chem Lett 9: 863-8 (1999)

Merck Research Laboratories

2D 3D TSV

10206550

Bicyclo[3.2.1]octanes: synthesis and inhibition of binding at the dopamine and serotonin transporters.

Bioorg Med Chem Lett 9: 857-62 (1999)

Organix Inc

2D 3D TSV

10206549

Synthesis and activity of gamma-(L-gamma-azaglutamyl)-S-(p-bromobenzyl)-L-cysteinylglycine: a metabolically stable inhibitor of glyoxalase I.

Bioorg Med Chem Lett 9: 853-6 (1999)

University of Minnesota

2D 3D TSV

10206548

Novel reverse-turn mimics inhibit farnesyl transferase.

Bioorg Med Chem Lett 9: 847-52 (1999)

Cold Spring Harbor Laboratory

2D 3D TSV

10206547

Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid.

Bioorg Med Chem Lett 9: 841-6 (1999)

Universit£t Erlangen-N£rnberg

2D 3D TSV

10206546

Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications.

Bioorg Med Chem Lett 9: 835-40 (1999)

Warner-Lambert Company

2D 3D TSV

10206545

Ring constrained analogues of the orvinols: the furanomorphides.

Bioorg Med Chem Lett 9: 831-4 (1999)

University of Bristol

2D 3D TSV

10206542

Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.

Bioorg Med Chem Lett 9: 815-20 (1999)

Warner-Lambert Company

2D 3D TSV

10206539

A new class of anti-HIV agents: synthesis and activity of conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor.

Bioorg Med Chem Lett 9: 803-6 (1999)

Kyoto Pharmaceutical University

2D 3D TSV

10201849

Synthesis of alpha-C(1-->3)-mannopyranoside of N-acetylgalactosamine, a new beta-galactosidase inhibitor.

Bioorg Med Chem Lett 9: 793-6 (1999)

Institut de chimie organique de l'Université de Lausanne

2D 3D TSV

10201846

Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 2. Sidechain optimization and demonstration of in vivo efficacy.

Bioorg Med Chem Lett 9: 775-80 (1999)

Eli Lilly and Company

2D 3D TSV

10201844

Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists.

Bioorg Med Chem Lett 9: 765-70 (1999)

Agouron Pharmaceuticals Inc

2D 3D TSV

10201842

Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.

Bioorg Med Chem Lett 9: 755-8 (1999)

Merck Research Laboratories

2D 3D TSV

10201841

Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.

Bioorg Med Chem Lett 9: 749-54 (1999)

Merck Research Laboratories

2D 3D TSV

10201840

A new class of potent RAR antagonists: dihydroanthracenyl, benzochromenyl and benzothiochromenyl retinoids.

Bioorg Med Chem Lett 9: 743-8 (1999)

Allergan Inc

2D 3D TSV

10201839

Studies towards the identification of potent, selective and bioavailable thrombin inhibitors.

Bioorg Med Chem Lett 9: 737-42 (1999)

Novartis Horsham Research Center

2D 3D TSV

10201832

Potent inhibitors of protein farnesyltransferase: heteroarenes as cysteine replacements.

Bioorg Med Chem Lett 9: 703-8 (1999)

Abbott Laboratories

2D 3D TSV

10201830

First hydroxamate inhibitors for carboxypeptidase A. N-acyl-N-hydroxy-beta-phenylalanines.

Bioorg Med Chem Lett 9: 691-6 (1999)

Pohang University of Science and Technology

2D 3D TSV

10201829

1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.

Bioorg Med Chem Lett 9: 685-90 (1999)

NV Organon

2D 3D TSV

10201827

Synthesis and activity of 2-(sulfonamido)methyl-carbapenems: discovery of a novel, anti-MRSA 1,8-naphthosultam pharmacophore.

Bioorg Med Chem Lett 9: 673-8 (1999)

Merck Research Laboratories

2D 3D TSV

10201826

Synthesis of oxytocin antagonists containing conformationally constrained amino acids in position 2.

Bioorg Med Chem Lett 9: 667-72 (1999)

Albert Szent-Gy£rgyi Medical University

2D 3D TSV

10201825

Solid-phase synthesis of benzisothiazolones as serine protease inhibitors.

Bioorg Med Chem Lett 9: 663-6 (1999)

Bristol-Myers Squibb Pharmaceutical Research Institute

2D 3D TSV

10201822

Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists.

Bioorg Med Chem Lett 9: 647-52 (1999)

Eli Lilly and Company

2D 3D TSV

10201821

Potent, orally absorbed glucagon receptor antagonists.

Bioorg Med Chem Lett 9: 641-6 (1999)

Merck Research Laboratories

2D 3D TSV

166

10198227

PSC833, cyclosporin A, and dexniguldipine effects on cellular calcein retention and inhibition of the multidrug resistance pump in human leukemic lymphoblasts.

Biochem Biophys Res Commun 257: 410-3 (1999)

University of Tennessee Medical Center

2D 3D TSV

10197974

Fluorescent pseudo-peptide linear vasopressin antagonists: design, synthesis, and applications.

J Med Chem 42: 1312-9 (1999)

University of Montpellier

2D 3D TSV

10197973

Quinuclidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase: optimization from lipid profiles.

J Med Chem 42: 1306-11 (1999)

Zeneca Pharmaceuticals

2D 3D TSV

10197972

1-Arylnaphthalene lignan: a novel scaffold for type 5 phosphodiesterase inhibitor.

J Med Chem 42: 1293-305 (1999)

Tanabe Seiyaku Company, Ltd.

2D 3D TSV

133

10197970

2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.

J Med Chem 42: 1274-81 (1999)

Merck Frosst Centre for Therapeutic Research

2D 3D TSV

10197969

Enzyme-assisted total synthesis of the optical antipodes D-myo-inositol 3,4,5-trisphosphate and D-myo-inositol 1,5, 6-trisphosphate: aspects of their structure-activity relationship to biologically active inositol phosphates.

J Med Chem 42: 1262-73 (1999)

Bergische Universität Wuppertal

2D 3D TSV

10197967

Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors.

J Med Chem 42: 1235-49 (1999)

Boehringer Ingelheim Pharma KG

2D 3D TSV

10197965

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 4. Incorporation of P1 lactam moieties as L-glutamine replacements.

J Med Chem 42: 1213-24 (1999)

Agouron Pharmaceuticals Inc

2D 3D TSV

10197964

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 3. Structure-activity studies of ketomethylene-containing peptidomimetics.

J Med Chem 42: 1203-12 (1999)

Agouron Pharmaceuticals Inc

2D 3D TSV

10197963

Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-Amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives.

J Med Chem 42: 1193-202 (1999)

University of Kuopio

2D 3D TSV

10197962

Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.

J Med Chem 42: 1178-92 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10197960

Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series.

J Med Chem 42: 1161-9 (1999)

Warner-Lambert Company

2D 3D TSV

171

10197959

J Med Chem 42: 1151-60 (1999)

Warner-Lambert Company

2D 3D TSV

10197956

Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)- and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine.

J Med Chem 42: 1115-22 (1999)

Vrije Universiteit

2D 3D TSV

10196521

Molecular identification of the corticosterone-sensitive extraneuronal catecholamine transporter.

Nat Neurosci 1: 349-51 (1999)

University of Heidelberg

2D 3D TSV

10188979

ATP- and glutathione-dependent transport of chemotherapeutic drugs by the multidrug resistance protein MRP1.

Br J Pharmacol 126: 681-8 (1999)

University Hospital Groningen

2D 3D TSV

10098677

Solid-phase synthesis of novel inhibitors of farnesyl transferase.

Bioorg Med Chem Lett 9: 623-6 (1999)

Institute of Cancer Research

2D 3D TSV

10098676

Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists.

Bioorg Med Chem Lett 9: 619-22 (1999)

Merck KGaA

2D 3D TSV

10098675

Homoisofagomines: chemical-enzymatic synthesis and evaluation as alpha- and beta-glucosidase inhibitors.

Bioorg Med Chem Lett 9: 615-8 (1999)

Technische Universit£t Berlin

2D 3D TSV

10098670

Stereoselective synthesis and receptor activity of conformationally defined retinoid X receptor selective ligands.

Bioorg Med Chem Lett 9: 589-94 (1999)

Allergan Inc

2D 3D TSV

10098669

Synthesis and sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands.

Bioorg Med Chem Lett 9: 585-8 (1999)

Merck Sharp & Dohme Research Laboratories

2D 3D TSV

10098666

High affinity retinoic acid receptor antagonists: analogs of AGN 193109.

Bioorg Med Chem Lett 9: 573-6 (1999)

Allergan Inc

2D 3D TSV

10098663

Nonpeptide small-molecular inhibitors of dipeptidyl peptidase IV: N-phenylphthalimide analogs.

Bioorg Med Chem Lett 9: 559-62 (1999)

University of Tokyo

2D 3D TSV

10098661

Inhibition of 4-hydroxyphenylpyruvate dioxygenase by sethoxydim, a potent inhibitor of acetyl-coenzyme A carboxylase.

Bioorg Med Chem Lett 9: 551-4 (1999)

Tunghai Christian University

2D 3D TSV

10098659

Synthesis of 5,8-dimethoxy-3-hydroxy-4-quinolone, a reported inhibitor of HIV RT, and evidence the original proposed structure was incorrect.

Bioorg Med Chem Lett 9: 543-6 (1999)

MediChem Research, Inc.

2D 3D TSV

10098657

(3-substituted benzyl)thiazolidine-2,4-diones as structurally new antihyperglycemic agents.

Bioorg Med Chem Lett 9: 533-8 (1999)

Kyorin Pharmaceutical Co., Ltd

2D 3D TSV

10098656

Synthesis and biological evaluation of alpha,alpha-difluorobenzylphosphonic acid derivatives as small molecular inhibitors of protein-tyrosine phosphatase 1B.

Bioorg Med Chem Lett 9: 529-32 (1999)

Tokyo University of Pharmacy & Life Science

2D 3D TSV

10098655

Novel nonsteroidal selective estrogen receptor modulators. Carbon and heteroatom replacement of oxygen in the ethoxypiperidine region of raloxifene.

Bioorg Med Chem Lett 9: 523-8 (1999)

Eli Lilly and Company

2D 3D TSV

10096862

bis-5-Alkylresorcinols from Panopsis rubescens that inhibit DNA polymerase beta.

J Nat Prod 62: 477-80 (1999)

University of Virginia

2D 3D TSV

10096852

New phenolic and quinone-methide triterpenes from Maytenus amazonica.

J Nat Prod 62: 434-6 (1999)

Universidad de La Laguna

2D 3D TSV

10091708

Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.

Bioorg Med Chem Lett 9: 491-6 (1999)

Merck Research Laboratories

2D 3D TSV

10091706

Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.

Bioorg Med Chem Lett 9: 481-6 (1999)

University of Kansas

2D 3D TSV

176

10091705

Structure-activity relationships of a series of benzothiophene-derived NPY Y1 antagonists: optimization of the C-2 side chain.

Bioorg Med Chem Lett 9: 475-80 (1999)

Eli Lilly and Company

2D 3D TSV

10091703

The design of non-peptide human bradykinin B2 receptor antagonists employing the benzodiazepine peptidomimetic scaffold.

Bioorg Med Chem Lett 9: 463-8 (1999)

Novartis Institute for Medical Sciences

2D 3D TSV

10091702

Cleavage of the cyclohexyl-subunit of rapamycin results in loss of immunosuppressive activity.

Bioorg Med Chem Lett 9: 459-62 (1999)

Novartis Pharma AG

2D 3D TSV

10091700

Inhibition of human cytomegalovirus protease by enedione derivatives of thieno[2,3-d]oxazinones through a novel dual acylation/alkylation mechanism.

Bioorg Med Chem Lett 9: 449-52 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10091699

Inhibition of herpes proteases and antiviral activity of 2-substituted thieno[2,3-d]oxazinones.

Bioorg Med Chem Lett 9: 443-8 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10091698

Automated parallel synthesis of a tetrahydroisoquinolin-based library: potential prolyl endopeptidase inhibitors.

Bioorg Med Chem Lett 9: 437-42 (1999)

Université de Lille II

2D 3D TSV

10091697

Synthetic [5,5] trans-fused indane lactones as inhibitors of thrombin.

Bioorg Med Chem Lett 9: 431-6 (1999)

Glaxo Wellcome Research and Development

2D 3D TSV

10091694

Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.

Bioorg Med Chem Lett 9: 413-8 (1999)

Nippon Steel Corporation

2D 3D TSV

10091693

The synthesis and evaluation of temperature sensitive tubulin toxins.

Bioorg Med Chem Lett 9: 407-12 (1999)

University of Virginia

2D 3D TSV

10091692

Synthesis and thromboxane A2 antagonistic activity activity of indane derivatives.

Bioorg Med Chem Lett 9: 401-6 (1999)

Zeria Pharmaceutical Co., Ltd.

2D 3D TSV

10091687

Synthesis and structure-activity relationships of a series of novel thiazoles as inhibitors of aminoacyl-tRNA synthetases.

Bioorg Med Chem Lett 9: 375-80 (1999)

Cubist Pharmaceuticals Inc

2D 3D TSV

10091684

The LMC delta opioid recognition pharmacophore: comparison of SNC80 and oxymorphindole.

Bioorg Med Chem Lett 9: 357-62 (1999)

National Institute of Diabetes

2D 3D TSV

10091683

Periodinates: a new class of protein tyrosine phosphatase inhibitors.

Bioorg Med Chem Lett 9: 353-6 (1999)

McGill University

2D 3D TSV

10091682

Monocarboxylic-based phosphotyrosyl mimetics in the design of GRB2 SH2 domain inhibitors.

Bioorg Med Chem Lett 9: 347-52 (1999)

National Cancer Institute-Bethesda

2D 3D TSV

10091679

New selective nonsteroidal aromatase inhibitors: synthesis and inhibitory activity of 2,3 or 5-(alpha-azolylbenzyl)-1H-indoles.

Bioorg Med Chem Lett 9: 333-6 (1999)

Nantes

2D 3D TSV

10091678

Novel series of O-substituted 8-quinolines and 4-benzothiazoles as potent antagonists of the bradykinin B2 receptors.

Bioorg Med Chem Lett 9: 327-32 (1999)

Hoechst Marion Roussel Inc

2D 3D TSV

10091677

Substituted furans as inhibitors of the PDE4 enzyme.

Bioorg Med Chem Lett 9: 323-6 (1999)

Merck Frosst Centre for Therapeutic Research

2D 3D TSV

10091675

Carbohydroxamido-oxazolidines: antibacterial agents that target lipid A biosynthesis.

Bioorg Med Chem Lett 9: 313-8 (1999)

Merck Research Laboratories

2D 3D TSV

10091674

Structure-based design of COX-2 selectivity into flurbiprofen.

Bioorg Med Chem Lett 9: 307-12 (1999)

Merck Frosst Canada Inc.

2D 3D TSV

10091673

Synthesis of potent and selective inhibitors of human plasma kallikrein.

Bioorg Med Chem Lett 9: 301-6 (1999)

The Procter & Gamble Company

2D 3D TSV

10090793

Thieno[3,2-b]- and thieno[2,3-b]pyrrole bioisosteric analogues of the hallucinogen and serotonin agonist N,N-dimethyltryptamine.

J Med Chem 42: 1106-11 (1999)

Purdue University

2D 3D TSV

10090792

Melatonergic properties of the (+)- and (-)-enantiomers of N-(4-methoxy-2,3-dihydro-1H-phenalen-2-yl)amide derivatives.

J Med Chem 42: 1100-5 (1999)

Universit£ de Paris-Sud

2D 3D TSV

10090791

Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.

J Med Chem 42: 1088-99 (1999)

Tanabe Seiyaku Company, Ltd.

2D 3D TSV

10090790

Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs.

J Med Chem 42: 1076-87 (1999)

Taisho Pharmaceutical Company Ltd

2D 3D TSV

131

10090788

Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).

J Med Chem 42: 1053-65 (1999)

SmithKline Beecham S.p.A.

2D 3D TSV

10090787

Structure-activity relationship of diaryl phosphonate esters as potent irreversible dipeptidyl peptidase IV inhibitors.

J Med Chem 42: 1041-52 (1999)

University of Antwerp (UIA)

2D 3D TSV

10090786

Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors

J Med Chem 42: 1027-40 (1999)

Eli Lilly and Company

2D 3D TSV

10090785

Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.

J Med Chem 42: 1018-26 (1999)

NOVARTIS Limited

2D 3D TSV

10090784

Synthesis and antiparasitic and antitumor activity of 2, 4-diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline analogues of piritrexim.

J Med Chem 42: 1007-17 (1999)

Harvard Medical School

2D 3D TSV

10090780

Structural and conformational requirements for high-affinity binding to the SH2 domain of Grb2(1).

J Med Chem 42: 971-80 (1999)

Novartis Forschungsinstitut

2D 3D TSV

10090778

Design, synthesis, and evaluation of conformationally constrained tongs, new inhibitors of HIV-1 protease dimerization.

J Med Chem 42: 957-62 (1999)

Université de Paris-Sud

2D 3D TSV

10090777

Novel inhibitors of carboxypeptidase G2 (CPG2): potential use in antibody-directed enzyme prodrug therapy.

J Med Chem 42: 951-6 (1999)

Imperial College

2D 3D TSV

10087037

Interactions of a nonpeptidic drug, valacyclovir, with the human intestinal peptide transporter (hPEPT1) expressed in a mammalian cell line.

J Pharmacol Exp Ther 289: 448-54 (1999)

Rutgers University

2D 3D TSV

10087018

Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity.

J Pharmacol Exp Ther 289: 304-11 (1999)

University of Rochester

2D 3D TSV

10087012

Molecular and ligand-binding characterization of the sigma-receptor in the Jurkat human T lymphocyte cell line.

J Pharmacol Exp Ther 289: 251-60 (1999)

Medical College of Georgia

2D 3D TSV

10082798

Molecular mechanisms of organic cation transport in OCT2-expressing Xenopus oocytes.

Biochim Biophys Acta 1417: 224-31 (1999)

Kyoto University Hospital

2D 3D TSV

10081621

Erythromycin derivatives ABT 229 and GM 611 act on motilin receptors in the rabbit duodenum.

Clin Exp Pharmacol Physiol 26: 242-5 (1999)

University of Melbourne

2D 3D TSV

10075775

Sideroxylonal C, a new inhibitor of human plasminogen activator inhibitor type-1, from the flowers of Eucalyptus albens.

J Nat Prod 62: 324-6 (1999)

Griffith University

2D 3D TSV

10075763

Antioxidant and antiinflammatory activities of anthocyanins and their aglycon, cyanidin, from tart cherries.

J Nat Prod 62: 294-6 (1999)

Department of Horticulture and National Food Safety and Toxicology Center

2D 3D TSV

10075742

New bioactive flavonoids and stilbenes in cubé resin insecticide.

J Nat Prod 62: 205-10 (1999)

University of California

2D 3D TSV

10072689

Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses.

J Med Chem 42: 920-34 (1999)

Biogen Inc

2D 3D TSV

10072688

Identification of novel classes of protein kinase inhibitors using combinatorial peptide chemistry based on functional genomics knowledge.

J Med Chem 42: 910-9 (1999)

Northwestern University

2D 3D TSV

10072687

Design, synthesis, and structure-activity relationships of acetylene-based histamine H3 receptor antagonists.

J Med Chem 42: 903-9 (1999)

Gliatech Inc

2D 3D TSV

10072686

Substrate specificity and stereoselectivity of rat brain microsomal anandamide amidohydrolase.

J Med Chem 42: 896-902 (1999)

University of Connecticut

2D 3D TSV

10072685

Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-(aminomethyl)-3-phenylbicyclo[2.2.2]- and -[2.2.1]alkane dopamine uptake inhibitors.

J Med Chem 42: 882-95 (1999)

Georgia Institute of Technology

2D 3D TSV

10072684

Prediction of the binding free energies of new TIBO-like HIV-1 reverse transcriptase inhibitors using a combination of PROFEC, PB/SA, CMC/MD, and free energy calculations.

J Med Chem 42: 868-81 (1999)

University of California San Francisco

2D 3D TSV

10072683

Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase.

J Med Chem 42: 859-67 (1999)

Emory University

2D 3D TSV

10072682

Bisquaternary ligands of the common allosteric site of M2 acetylcholine receptors: search for the minimum essential distances between the pharmacophoric elements.

J Med Chem 42: 849-58 (1999)

University of Bonn

2D 3D TSV

10072681

Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines.

J Med Chem 42: 833-48 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

113

10072680

Corticotropin-releasing hormone receptor antagonists: framework design and synthesis guided by ligand conformational studies.

J Med Chem 42: 819-32 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10072679

Non-peptide corticotropin-releasing hormone antagonists: syntheses and structure-activity relationships of 2-anilinopyrimidines and -triazines.

J Med Chem 42: 805-18 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

10072676

Acquisition of high-affinity, SH2-targeted ligands via a spatially focused library.

J Med Chem 42: 784-7 (1999)

The Albert Einstein College of Medicine of Yeshiva University

2D 3D TSV

10072675

Discovery of 6-oxo-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1(6H)- pyridazinebutanoic acid (FK 838): a novel non-xanthine adenosine A1 receptor antagonist with potent diuretic activity.

J Med Chem 42: 779-83 (1999)

Fujisawa Pharmaceutical Company, Ltd.

2D 3D TSV

10052994

CHO/hPEPT1 cells overexpressing the human peptide transporter (hPEPT1) as an alternative in vitro model for peptidomimetic drugs.

J Pharm Sci 88: 347-50 (1999)

The University of Michigan

2D 3D TSV

10052983

Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.

J Med Chem 42: 769-76 (1999)

University of Connecticut

2D 3D TSV

10052980

Synthesis of retinoid X receptor-specific ligands that are potent inducers of adipogenesis in 3T3-L1 cells.

J Med Chem 42: 742-50 (1999)

Ligand Pharmaceuticals Inc

2D 3D TSV

138

10052979

Aminopyridazines as acetylcholinesterase inhibitors.

J Med Chem 42: 730-41 (1999)

Universit£ Louis Pasteur

2D 3D TSV

10052978

Phosphotyrosine-containing dipeptides as high-affinity ligands for the p56lck SH2 domain.

J Med Chem 42: 722-9 (1999)

Boehringer Ingelheim Pharmaceuticals Inc

2D 3D TSV

10052977

Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.

J Med Chem 42: 706-21 (1999)

National Institute of Diabetes

2D 3D TSV

10052976

3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.

J Med Chem 42: 691-705 (1999)

Merck Sharp and Dohme Research Laboratories

2D 3D TSV

126

10052975

Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.

J Med Chem 42: 677-90 (1999)

Merck Sharp and Dohme Research Laboratories

2D 3D TSV

129

10052973

Cycloalkanecarboxylic esters derived from lysergol, dihydrolysergol-I, and elymoclavine as partial agonists and antagonists at rat 5-HT2A receptors: pharmacological evidence that the indolo[4,3-fg]quinoline system of the ergolines is responsible for high 5-HT2A receptor affinity.

J Med Chem 42: 659-68 (1999)

Freie Universit£t Berlin

2D 3D TSV

10052970

Design, synthesis, and dopamine receptor modulating activity of spiro bicyclic peptidomimetics of L-prolyl-L-leucyl-glycinamide.

J Med Chem 42: 628-37 (1999)

University of Minnesota

2D 3D TSV

10052969

5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.

J Med Chem 42: 619-27 (1999)

Sapienza University of Rome

2D 3D TSV

10052968

Design and synthesis of novel amphiphilic dendritic galactosides for selective targeting of liposomes to the hepatic asialoglycoprotein receptor.

J Med Chem 42: 609-18 (1999)

Leiden University

2D 3D TSV

10052967

Bicyclic tripeptide mimetics with reverse turn inducing properties.

J Med Chem 42: 601-8 (1999)

Uppsala University

2D 3D TSV

10052966

Development of chiral N-alkylcarbamates as new leads for potent and selective H3-receptor antagonists: synthesis, capillary electrophoresis, and in vitro and oral in vivo activity.

J Med Chem 42: 593-600 (1999)

Freie Universität Berlin

2D 3D TSV

10052965

Syntheses and biological activities of rebeccamycin analogues. Introduction of a halogenoacetyl substituent.

J Med Chem 42: 584-92 (1999)

Universit£ Blaise Pascal

2D 3D TSV

10052963

New peptidic cysteine protease inhibitors derived from the electrophilic alpha-amino acid aziridine-2,3-dicarboxylic acid.

J Med Chem 42: 560-72 (1999)

Albert-Ludwigs-University of Freiburg

2D 3D TSV

10052962

Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists.

J Med Chem 42: 545-59 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10052961

Dual inhibition of phosphodiesterase 4 and matrix metalloproteinases by an (arylsulfonyl)hydroxamic acid template.

J Med Chem 42: 541-4 (1999)

Rhône-Poulenc Rorer

2D 3D TSV

10052959

Tetrahydrobenzindoles: selective antagonists of the 5-HT7 receptor.

J Med Chem 42: 533-5 (1999)

Meiji Seika Kaisha Ltd.

2D 3D TSV

10051134

[3H]-Mesulergine labels 5-HT7 sites in rat brain and guinea-pig ileum but not rat jejunum.

Br J Pharmacol 126: 179-88 (1999)

Monash University

2D 3D TSV

10048786

Effects of the indolocarbazole 3744W on the tyrosine kinase activity of the cytoplasmic domain of the platelet-derived growth factor beta-receptor.

Cell Signal 11: 95-100 (1999)

Wellcome Research Laboratories

2D 3D TSV

10027858

The interaction of n-tetraalkylammonium compounds with a human organic cation transporter, hOCT1.

J Pharmacol Exp Ther 288: 1192-8 (1999)

University of California San Francisco

2D 3D TSV

10021947

4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists.

Bioorg Med Chem Lett 9: 291-4 (1999)

Merck & Co.

2D 3D TSV

10021946

Identification of (-)-cis-6-acetyl-4S-(3-chloro-4-fluoro-benzoylamino)- 3,4-dihydro-2,2-dimethyl-2H-benzo[b]pyran-3S-ol as a potential antimigraine agent.

Bioorg Med Chem Lett 9: 285-90 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10021945

Photoactivatable peptides based on BMS-197525: a potent antagonist of the human thrombin receptor (PAR-1).

Bioorg Med Chem Lett 9: 279-84 (1999)

University at Stony Brook

2D 3D TSV

10021944

Specific, uncompetitive inhibition of beta-galactosidases by a 5,6-isopropylidenedioxyfuro[2,3-d]isoxazole-3-methanol derivative.

Bioorg Med Chem Lett 9: 277-8 (1999)

Institut de chimie organique de l'Université de Lausanne

2D 3D TSV

10021942

Trifluoromethyl ketone inhibitors of fatty acid amide hydrolase: a probe of structural and conformational features contributing to inhibition.

Bioorg Med Chem Lett 9: 265-70 (1999)

Scripps Research Institute

2D 3D TSV

10021941

Synthesis and PLA2-inhibitory properties of 2(R)-acetamido-alkylphosphomethanols with a variable aggregate anchor.

Bioorg Med Chem Lett 9: 261-4 (1999)

Tumor Biology Center

2D 3D TSV

10021933

Highly potent inhibitors of the Grb2-SH2 domain.

Bioorg Med Chem Lett 9: 221-6 (1999)

Novartis Pharma Inc

2D 3D TSV

10021927

Design and synthesis of thiol containing inhibitors of matrix metalloproteinases.

Bioorg Med Chem Lett 9: 195-200 (1999)

Novartis Biomedical Research Institute

2D 3D TSV

10021923

Novel 1,2,3,4-tetrahydroisoquinolines with high affinity and selectivity for the dopamine D3 receptor.

Bioorg Med Chem Lett 9: 179-84 (1999)

SmithKline Beecham Pharmaceuticals Ltd

2D 3D TSV

10021922

Synthesis, computer modeling and biological evaluation of novel protein kinase C agonists based on a 7-membered lactam moiety.

Bioorg Med Chem Lett 9: 173-8 (1999)

University of Tokyo

2D 3D TSV

10021918

Substituted heterocyclic analogs as selective COX-2 inhibitors in the flosulide class.

Bioorg Med Chem Lett 9: 151-6 (1999)

Merck Frosst Centre for Therapeutic Research

2D 3D TSV

10021917

Indolocarbazole poisons of human topoisomerase I: regioisomeric analogues of ED-110.

Bioorg Med Chem Lett 9: 145-50 (1999)

MediChem Research, Inc.

2D 3D TSV

10021916

Synthesis and sulfatase inhibitory activities of (E)- and (Z)-4-hydroxytamoxifen sulfamates.

Bioorg Med Chem Lett 9: 141-4 (1999)

Duquesne University

2D 3D TSV

10021915

The synthesis of ketomethylene pseudopeptide analogues of dipeptide aldehyde inhibitors of calpain.

Bioorg Med Chem Lett 9: 139-40 (1999)

Hoechst Marion Roussel Inc

2D 3D TSV

10021913

Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket.

Bioorg Med Chem Lett 9: 127-32 (1999)

Pfizer Inc

2D 3D TSV

10021912

Isoxazoline GPIIb/IIIa antagonists bearing a phosphoramidate.

Bioorg Med Chem Lett 9: 123-6 (1999)

DuPont Pharmaceuticals Company

2D 3D TSV

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