Search by PubMed Identification
PMID | Data | Article Title | Citation | Organization | Data Download |
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7996555 | 5 | Bis-catechol-substituted redox-reactive analogues of hexamethonium and decamethonium: stimulated affinity-dependent reactivity through iron peroxide catalysis. | J Med Chem 37: 4417-20 (1995) | University of Toledo | 2D 3D TSV |
7996550 | 12 | Development of a model for the delta opioid receptor pharmacophore. 2. Conformationally restricted Phe3 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13). | J Med Chem 37: 4384-91 (1995) | University of Michigan | 2D 3D TSV |
7996549 | 40 | Development of a model for the delta opioid receptor pharmacophore. 1. Conformationally restricted Tyr1 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13). | J Med Chem 37: 4371-83 (1995) | University of Michigan | 2D 3D TSV |
7996545 | 3 | 1-(2,5-Dimethoxy-4-(trifluoromethyl)phenyl)-2-aminopropane: a potent serotonin 5-HT2A/2C agonist. | J Med Chem 37: 4346-51 (1995) | Purdue University | 2D 3D TSV |
7996543 | 32 | Synthesis and molecular modeling of 1-phenyl-1,2,3,4-tetrahydroisoquinolines and related 5,6,8,9-tetrahydro-13bH-dibenzo[a,h]quinolizines as D1 dopamine antagonists. | J Med Chem 37: 4317-28 (1995) | University of North Carolina | 2D 3D TSV |
7996542 | 32 | N6-substituted adenosine receptor agonists. Synthesis and pharmacological activity as potent antinociceptive agents. | J Med Chem 37: 4307-16 (1995) | Carpibem | 2D 3D TSV |
7996541 | 12 | Synthesis, in vitro biological stability, and anti-HIV activity of 5-halo-6-alkoxy(or azido)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs to 3'-azido-3'-deoxythymidine (AZT). | J Med Chem 37: 4297-306 (1995) | University of Alberta | 2D 3D TSV |
7996538 | 42 | Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol. | J Med Chem 37: 4270-7 (1995) | University of Washington | 2D 3D TSV |
7996470 | 29 | The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors. | J Pharmacol Exp Ther 271: 1558-65 (1994) | University of Michigan | 2D 3D TSV |
7990927 | 13 | Drug excretion mediated by a new prototype of polyspecific transporter. | Nature 372: 549-552 (1994) | Bayerische Julius-Maximilians-Universit£t | 2D 3D TSV |
7990124 | 11 | Studies of the active conformation of a novel series of benzamide dopamine D2 agonists. | J Med Chem 37: 4251-7 (1995) | Warner-Lambert Company | 2D 3D TSV |
7990123 | 30 | Iodinated 2-aminotetralins and 3-amino-1-benzopyrans: ligands for dopamine D2 and D3 receptors. | J Med Chem 37: 4245-50 (1995) | University of Pennsylvania | 2D 3D TSV |
7990119 | 91 | Structure-activity relationships and pH dependence of binding of 8-alkyl-N5-deazapterins to dihydrofolate reductase. | J Med Chem 37: 4211-21 (1995) | University of Sydney | 2D 3D TSV |
7990111 | 35 | Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor. | J Med Chem 37: 4109-17 (1995) | University of North Carolina | 2D 3D TSV |
7990110 | 57 | A comparative molecular field analysis model for 6-arylpyrrolo[2,1-d] [1,5]benzothiazepines binding selectively to the mitochondrial benzodiazepine receptor. | J Med Chem 37: 4100-8 (1995) | Universit£ di Napoli | 2D 3D TSV |
7990109 | 62 | Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity. | J Med Chem 37: 4085-99 (1995) | H. Lundbeck A/S | 2D 3D TSV |
7990108 | 8 | Novel antiproliferative agents derived from lavendustin A. | J Med Chem 37: 4079-84 (1995) | Sandoz Research Institute | 2D 3D TSV |
7990107 | 3 | Multisubstrate inhibition of 4-hydroxybenzoate 3-monooxygenase. | J Med Chem 37: 4076-8 (1995) | Marion Merrell Dow Research Institute | 2D 3D TSV |
7990105 | 16 | A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist. | J Med Chem 37: 4068-72 (1995) | Merck Research Laboratories | 2D 3D TSV |
7990104 | 15 | The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential. | J Med Chem 37: 4053-67 (1995) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
7988476 | 136 | Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5). | Endocrinology 135: 2814-7 (1994) | McGill University | 2D 3D TSV |
7984267 | 675 | Molecular biology of 5-HT receptors. | Neuropharmacology 33: 275-317 (1994) | University of Alberta | 2D 3D TSV |
7969084 | 5 | Biological properties of the benzodiazepine amidine derivative L-740,093, a cholecystokinin-B/gastrin receptor antagonist with high affinity in vitro and high potency in vivo. | Mol Pharmacol 46: 943-8 (1994) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
7966163 | 74 | Structure-activity relationships of C1 and C6 side chains of zaragozic acid A derivatives. | J Med Chem 37: 4031-51 (1994) | Merck Research Laboratories | 2D 3D TSV |
7966162 | 39 | Selective ligands for rat A3 adenosine receptors: structure-activity relationships of 1,3-dialkylxanthine 7-riboside derivatives. | J Med Chem 37: 4020-30 (1994) | National Institute of Diabetes | 2D 3D TSV |
7966161 | 45 | Cephem sulfones as inactivators of human leukocyte elastase. 5. 7 alpha-Methoxy- and 7 alpha-chloro-1,1-dioxocephem 4-ketones. | J Med Chem 37: 4003-19 (1994) | Pharmacia-Farmitalia Carlo Erba | 2D 3D TSV |
7966160 | 7 | PRO_LIGAND: an approach to de novo molecular design. 2. Design of novel molecules from molecular field analysis (MFA) models and pharmacophores. | J Med Chem 37: 3994-4002 (1994) | Proteus Molecular Design Ltd. | 2D 3D TSV |
7966154 | 15 | Nonpeptide angiotensin II receptor antagonists. Synthesis, in vitro activity, and molecular modeling studies of N-[(heterobiaryl)methyl] imidazoles. | J Med Chem 37: 3928-38 (1994) | Istituto Lusofarmaco | 2D 3D TSV |
7966152 | 57 | Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11. | J Med Chem 37: 3910-7 (1994) | University of Arizona | 2D 3D TSV |
7966150 | 60 | Design and synthesis of potent and highly selective thrombin inhibitors. | J Med Chem 37: 3889-901 (1994) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
7966148 | 40 | Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally active COX-2 inhibitors. | J Med Chem 37: 3878-81 (1994) | Searle Research & Development | 2D 3D TSV |
7966147 | 14 | Synthesis, cocaine receptor affinity, and dopamine uptake inhibition of several new 2 beta-substituted 3 beta-phenyltropanes. | J Med Chem 37: 3875-7 (1994) | University of New Orleans | 2D 3D TSV |
7966146 | 53 | 4,7 beta-Dimethyl-4-azacholestan-3-one (MK-386) and related 4-azasteroids as selective inhibitors of human type 1 5 alpha-reductase. | J Med Chem 37: 3871-4 (1994) | Merck Research Laboratories | 2D 3D TSV |
7966145 | 2 | (-)-11-Hydroxy-7'-isothiocyanato-1',1'-dimethylheptyl-delta 8-THC: a novel, high-affinity irreversible probe for the cannabinoid receptor in the brain. | J Med Chem 37: 3867-70 (1994) | University of Connecticut | 2D 3D TSV |
7966143 | 5 | Binding of fluorescent and spin-labeled C-terminal hirudin analogs to thrombin. | J Med Chem 37: 3855-8 (1994) | Ohio State University | 2D 3D TSV |
7966142 | 4 | Adenosine deaminase inhibitors. Synthesis and biological evaluation of putative metabolites of (+)-erythro-9-(2S-hydroxy-3R-nonyl)adenine. | J Med Chem 37: 3844-9 (1994) | University of Rhode Island | 2D 3D TSV |
7966139 | 6 | Peptide-linked 1,3-dialkyl-3-acyltriazenes: gastrin receptor directed antineoplastic alkylating agents. | J Med Chem 37: 3812-8 (1994) | National Cancer Institute-Frederick | 2D 3D TSV |
7966138 | 55 | 5-Phenyl-3-ureidobenzazepin-2-ones as cholecystokinin-B receptor antagonists. | J Med Chem 37: 3789-811 (1994) | Pfizer Inc | 2D 3D TSV |
7966137 | 52 | Construction of a molecular shape analysis-three-dimensional quantitative structure-analysis relationship for an analog series of pyridobenzodiazepinone inhibitors of muscarinic 2 and 3 receptors. | J Med Chem 37: 3775-88 (1994) | College of Pharmacy | 2D 3D TSV |
7966134 | 1 | Generally applicable, convenient solid-phase synthesis and receptor affinities of octreotide analogs. | J Med Chem 37: 3749-57 (1994) | Washington University School of Medicine | 2D 3D TSV |
7966131 | 34 | Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors: heterocyclic ring systems containing P1' and P2' substituents. | J Med Chem 37: 3707-16 (1994) | Glaxo Research and Development Limited | 2D 3D TSV |
7966130 | 69 | Nitrogen-in-the-ring pyranoses and furanoses: structural basis of inhibition of mammalian glycosidases. | J Med Chem 37: 3701-6 (1994) | Hokuriku University | 2D 3D TSV |
7966128 | 2 | Design, synthesis, and conformational analysis of a novel macrocyclic HIV-protease inhibitor. | J Med Chem 37: 3684-92 (1994) | Marion Merrell Dow Research Institute | 2D 3D TSV |
7966126 | 3 | Improved binding affinity for cyclophilin A by a cyclosporin derivative singly modified at its effector domain. | J Med Chem 37: 3674-6 (1994) | Sandoz Pharma Ltd | 2D 3D TSV |
7966125 | 26 | A new class of non-peptidic cholecystokinin-B/gastrin receptor antagonists based on dibenzobicyclo[2.2.2]octane. | J Med Chem 37: 3671-3 (1994) | James Black Foundation | 2D 3D TSV |
7965790 | 38 | Species orthologs of the alpha-2A adrenergic receptor: the pharmacological properties of the bovine and rat receptors differ from the human and porcine receptors. | J Pharmacol Exp Ther 271: 735-40 (1994) | University of Nebraska | 2D 3D TSV |
7965765 | 14 | Cloning and pharmacologic characterization of a thromboxane A2 receptor from K562 (human chronic myelogenous leukemia) cells. | J Pharmacol Exp Ther 271: 1034-41 (1994) | University of Cincinnati | 2D 3D TSV |
7965746 | 33 | [125I]iodoproxyfan, a new antagonist to label and visualize cerebral histamine H3 receptors. | J Pharmacol Exp Ther 271: 452-9 (1994) | U. 109 | 2D 3D TSV |
7961706 | 2 | The MRP gene encodes an ATP-dependent export pump for leukotriene C4 and structurally related conjugates. | J Biol Chem 269: 27807-10 (1994) | Deutsches Krebsforschungszentrum | 2D 3D TSV |
7946354 | 11 | Cloning and characterization of a mammalian melatonin receptor that mediates reproductive and circadian responses. | Neuron 13: 1177-85 (1994) | Massachusetts General Hospital | 2D 3D TSV |
7945404 | 2 | Hepatobiliary elimination of the peroxisome proliferator nafenopin by conjugation and subsequent ATP-dependent transport across the canalicular membrane. | Biochem Pharmacol 48: 1113-20 (1994) | Deutsches Krebsforschungszentrum | 2D 3D TSV |
7932593 | 24 | Synthesis and 5-lipoxygenase inhibitory activities of some novel 2-substituted 5-benzofuran hydroxamic acids. | J Med Chem 37: 3663-7 (1994) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
7932591 | 69 | Three-dimensional molecular shape analysis-quantitative structure-activity relationship of a series of cholecystokinin-A receptor antagonists. | J Med Chem 37: 3639-54 (1994) | University of Illinois at Chicago | 2D 3D TSV |
7932590 | 29 | Influence of lipophilicity on the biological activity of cyclic pseudopeptide NK-2 receptor antagonists. | J Med Chem 37: 3630-8 (1994) | A. Menarini Industrie Farmaceutiche Riunite | 2D 3D TSV |
7932588 | 48 | 2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A3 adenosine receptors. | J Med Chem 37: 3614-21 (1994) | National Institute of Diabetes | 2D 3D TSV |
7932587 | 20 | Selective inhibition of trypanosomal glyceraldehyde-3-phosphate dehydrogenase by protein structure-based design: toward new drugs for the treatment of sleeping sickness. | J Med Chem 37: 3605-13 (1994) | University of Washington | 2D 3D TSV |
7932586 | 102 | Agents combining thromboxane receptor antagonism with thromboxane synthase inhibition: [[[2-(1H-imidazol-1-yl)ethylidene]amino]oxy]alkanoic acids. | J Med Chem 37: 3588-604 (1994) | Pharmacia-Farmitalia Carlo Erba | 2D 3D TSV |
7932585 | 5 | Nucleic acid related compounds. 84. Synthesis of 6'-(E and Z)-halohomovinyl derivatives of adenosine, inactivation of S-adenosyl-L-homocysteine hydrolase, and correlation of anticancer and antiviral potencies with enzyme inhibition. | J Med Chem 37: 3579-87 (1994) | Brigham Young University | 2D 3D TSV |
7932581 | 32 | The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents. | J Med Chem 37: 3523-33 (1994) | Parke-Davis Pharmaceutical Research | 2D 3D TSV |
7932580 | 53 | Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: synthesis and structure-activity relationship studies of a new series of trisubstituted imidazoles. | J Med Chem 37: 3511-22 (1994) | DuPont Pharmaceuticals Company | 2D 3D TSV |
7932578 | 20 | Synthesis and structure-activity relationships of peptidyl alpha-keto heterocycles as novel inhibitors of prolyl endopeptidase. | J Med Chem 37: 3492-502 (1994) | Meiji Seika Kaisha, Ltd | 2D 3D TSV |
7932577 | 24 | Selective kappa-opioid agonists: synthesis and structure-activity relationships of piperidines incorporating on oxo-containing acyl group. | J Med Chem 37: 3482-91 (1994) | SmithKline Beecham Farmaceutici S.p.A. | 2D 3D TSV |
7932576 | 20 | Structure-activity study of neuropeptide FF: contribution of N-terminal regions to affinity and activity. | J Med Chem 37: 3477-81 (1994) | CNRS | 2D 3D TSV |
7932573 | 19 | L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor. | J Med Chem 37: 3443-51 (1994) | Merck Research Laboratories | 2D 3D TSV |
7932572 | 7 | Structure-activity relationship studies of N-sulfonyl analogs of cocaine: role of ionic interaction in cocaine binding. | J Med Chem 37: 3440-2 (1994) | Trophix Pharmaceuticals, Inc. | 2D 3D TSV |
7932569 | 116 | Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in vivo properties. | J Med Chem 37: 3408-18 (1994) | Virginia Commonwealth University | 2D 3D TSV |
7932568 | 29 | Antitumor agents. 155. Synthesis and biological evaluation of 3',6,7-substituted 2-phenyl-4-quinolones as antimicrotubule agents. | J Med Chem 37: 3400-7 (1994) | University of North Carolina | 2D 3D TSV |
7932565 | 92 | Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors. | J Med Chem 37: 3373-82 (1994) | National Institute of Diabetes | 2D 3D TSV |
7932564 | 38 | Design, synthesis, and biological activity of methoctramine-related tetraamines bearing an 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4] benzodiazepin-6-one moiety: structural requirements for optimum occupancy of muscarinic receptor subtypes as revealed by symmetrical and unsymmetrical polyamines. | J Med Chem 37: 3363-72 (1994) | University of Bologna | 2D 3D TSV |
7932563 | 60 | Synthesis and biochemical evaluation of a series of aminoflavones as potential inhibitors of protein-tyrosine kinases p56lck, EGFr, and p60v-src. | J Med Chem 37: 3353-62 (1994) | Purdue University | 2D 3D TSV |
7932560 | 19 | (E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid and related compounds: high affinity leukotriene B4 receptor antagonists. | J Med Chem 37: 3327-36 (1994) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7932559 | 42 | Nonpeptidic inhibitors of human leukocyte elastase. 3. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of orally active 3-amino-6-phenylpyridin-2-one trifluoromethyl ketones. | J Med Chem 37: 3313-26 (1994) | Zeneca Pharmaceuticals Group | 2D 3D TSV |
7932558 | 30 | Nonpeptidic inhibitors of human leukocyte elastase. 2. Design, synthesis, and in vitro activity of a series of 3-amino-6-arylopyridin-2-one trifluoromethyl ketones. | J Med Chem 37: 3303-12 (1994) | Zeneca Pharmaceuticals Group | 2D 3D TSV |
7932557 | 25 | The synthesis and thymidylate synthase inhibitory activity of L-gamma-L-linked dipeptide and L-gamma-amide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583). | J Med Chem 37: 3294-302 (1994) | Institute of Cancer Research | 2D 3D TSV |
7932556 | 11 | Bicyclic hydantoins with a bridgehead nitrogen. Comparison of anticonvulsant activities with binding to the neuronal voltage-dependent sodium channel. | J Med Chem 37: 3289-93 (1994) | University of Alabama at Birmingham | 2D 3D TSV |
7932554 | 23 | The squalestatins: novel inhibitors of squalene synthase. Enzyme inhibitory activities and in vivo evaluation of C1-modified analogues. | J Med Chem 37: 3274-81 (1994) | Glaxo Research and Development Ltd. | 2D 3D TSV |
7932553 | 42 | 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. | J Med Chem 37: 3263-73 (1994) | Göteborg University | 2D 3D TSV |
7932552 | 18 | 3-Amino-5,5-dimethylhexanoic acid. Synthesis, resolution, and effects on carnitine acyltransferases. | J Med Chem 37: 3247-51 (1994) | University of Alabama at Birmingham | 2D 3D TSV |
7932551 | 5 | Synthesis and biological activity of bile acid-derived HMG-CoA reductase inhibitors. The role of 21-methyl in recognition of HMG-CoA reductase and the ileal bile acid transport system. | J Med Chem 37: 3240-6 (1994) | Hoechst AG | 2D 3D TSV |
7932550 | 92 | Synthesis and structure-activity relationships of novel naphthalenic and bioisosteric related amidic derivatives as melatonin receptor ligands. | J Med Chem 37: 3231-9 (1994) | Institut de Chimie Pharmaceutique | 2D 3D TSV |
7932546 | 5 | Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors. | J Med Chem 37: 3200-4 (1994) | Upjohn | 2D 3D TSV |
7932545 | 3 | (+)-1-(3S,4R)-[3-(4-phenylbenzyl)-4-hydroxychroman-7-yl]cyclopentane carboxylic acid, a highly potent, selective leukotriene B4 antagonist with oral activity in the murine collagen-induced arthritis model. | J Med Chem 37: 3197-9 (1994) | Pfizer Inc | 2D 3D TSV |
7932540 | 38 | A marked change of receptor affinity of the 2-methyl-5-(3-hydroxyphenyl)morphans upon attachment of an (E)-8-benzylidene moiety: synthesis and evaluation of a new class of sigma receptor ligands. | J Med Chem 37: 3163-70 (1994) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
7932538 | 54 | Docking analysis of a series of benzylamino acetylcholinesterase inhibitors with a phthalimide, benzoyl, or indanone moiety. | J Med Chem 37: 3141-53 (1994) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
7932536 | 13 | Molecular modeling studies of some choline acetyltransferase inhibitors. | J Med Chem 37: 3128-31 (1994) | University of North Carolina at Chapel Hill | 2D 3D TSV |
7932535 | 40 | Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. | J Med Chem 37: 3121-7 (1994) | National Taiwan University | 2D 3D TSV |
7932534 | 29 | Bromobenzofuran-based non-peptide antagonists of angiotensin II: GR138950, a potent antihypertensive agent with high oral bioavailability. | J Med Chem 37: 3108-20 (1994) | Glaxo Research and Development Ltd. | 2D 3D TSV |
7932533 | 11 | Rational design, synthesis, and crystallographic analysis of a hydroxyethylene-based HIV-1 protease inhibitor containing a heterocyclic P1'--P2' amide bond isostere. | J Med Chem 37: 3100-7 (1994) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7932532 | 23 | Non-peptidic inhibitors of human leukocyte elastase. 1. The design and synthesis of pyridone-containing inhibitors. | J Med Chem 37: 3090-9 (1994) | ZENECA Inc | 2D 3D TSV |
7932531 | 55 | Inhibitors of HIV-1 proteinase containing 2-heterosubstituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, enzyme inhibition, and antiviral activity. | J Med Chem 37: 3079-89 (1994) | SANDOZ Forschungsinstitut Ges.m.b.H. | 2D 3D TSV |
7932530 | 2 | Heteroaryl-fused 2-phenylisothiazolone inhibitors of cartilage breakdown. | J Med Chem 37: 3071-8 (1994) | DuPont Pharmaceuticals Company | 2D 3D TSV |
7932529 | 37 | Novel dual inhibitors of 5-lipoxygenase and thromboxane A2 synthetase: synthesis and structure-activity relationships of 3-pyridylmethyl-substituted 2-amino-6-hydroxybenzothiazole derivatives. | J Med Chem 37: 3062-70 (1994) | Eisai Company, Ltd | 2D 3D TSV |
7932524 | 38 | Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor. | J Med Chem 37: 3023-32 (1994) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
7932521 | 81 | Nonpeptide renin inhibitors with good intraduodenal bioavailability and efficacy in dog. | J Med Chem 37: 2991-3007 (1994) | Abbott Laboratories | 2D 3D TSV |
7932177 | 53 | Biochemical and pharmacological characterization of mu, delta and kappa 3 opioid receptors expressed in BE(2)-C neuroblastoma cells. | J Pharmacol Exp Ther 270: 1246-55 (1994) | Memorial Sloan-Kettering Cancer Center | 2D 3D TSV |
7925364 | 13 | Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene. | Eur J Biochem 224: 489-95 (1994) | Université Libre de Bruxelles | 2D 3D TSV |
7921604 | 16 | The effects of SB 204070, a highly potent and selective 5-HT4 receptor antagonist, on guinea-pig distal colon. | Br J Pharmacol 112: 789-94 (1994) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7915326 | 28 | Differential inhibition of aminopeptidase A and aminopeptidase N by new beta-amino thiols. | J Med Chem 37: 2950-7 (1994) | University of Paris | 2D 3D TSV |
7915318 | 120 | Biochemical and pharmacological characterization of high-affinity trimetoquinol analogs on guinea pig and human beta adrenergic receptor subtypes: evidence for partial agonism. | J Pharmacol Exp Ther 270: 665-74 (1994) | Ohio State University | 2D 3D TSV |
7914540 | 16 | Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone. | J Med Chem 37: 2564-73 (1994) | University of Santiago de Compostela | 2D 3D TSV |
7914539 | 36 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. | J Med Chem 37: 2552-63 (1994) | Burroughs Wellcome Company | 2D 3D TSV |
7914538 | 9 | Dopaminergic benzo[a]phenanthridines: resolution and pharmacological evaluation of the enantiomers of dihydrexidine, the full efficacy D1 dopamine receptor agonist. | J Med Chem 37: 2453-60 (1994) | Purdue University | 2D 3D TSV |
7914537 | 8 | A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors. | J Med Chem 37: 2328-33 (1994) | Ohio State University | 2D 3D TSV |
7914536 | 96 | Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. | J Med Chem 37: 2308-14 (1994) | Hoechst-Roussel Pharmaceuticals Inc | 2D 3D TSV |
7912735 | 270 | 3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies. | J Med Chem 37: 1779-93 (1994) | Universit£ d'Orl£ans | 2D 3D TSV |
7910217 | 36 | The [(methyloxy)imino]methyl moiety as a bioisoster of aryl. A novel class of completely aliphatic beta-adrenergic receptor antagonists. | J Med Chem 37: 1518-25 (1994) | Universitá di Pisa | 2D 3D TSV |
7910212 | 34 | Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo. | J Pharmacol Exp Ther 269: 725-31 (1994) | Yamanouchi Pharmaceutical Co., Ltd | 2D 3D TSV |
7909848 | 2 | A proposed model of bradykinin bound to the rat B2 receptor and its utility for drug design. | J Med Chem 37: 1347-54 (1994) | Scios Nova Inc | 2D 3D TSV |
7909847 | 33 | Investigation of the active site of aminopeptidase A using a series of new thiol-containing inhibitors. | J Med Chem 37: 1339-46 (1994) | University of Paris | 2D 3D TSV |
7909336 | 27 | A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. | J Med Chem 37: 1060-2 (1994) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
7908696 | 45 | Enkephalin analogs as systemically active antinociceptive agents: O- and N-alkylated derivatives of the dipeptide amide L-2,6-dimethyltyrosyl-N-(3-phenylpropyl)-D-alaninamide. | J Med Chem 37: 888-96 (1994) | Searle | 2D 3D TSV |
7908055 | 157 | Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. | J Pharmacol Exp Ther 268: 1403-10 (1994) | Case Western Reserve University | 2D 3D TSV |
7908054 | 71 | Characterization of [3H]RX821002 binding to alpha-2 adrenergic receptor subtypes. | J Pharmacol Exp Ther 268: 1362-7 (1994) | University of Nebraska | 2D 3D TSV |
7907148 | 32 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. | J Med Chem 37: 519-25 (1994) | University of Li£ge | 2D 3D TSV |
7905926 | 66 | Piperidinyltetralin sigma ligands. | J Med Chem 37: 364-70 (1994) | DuPont Pharmaceuticals Company | 2D 3D TSV |
7904648 | 3 | Studies on antiulcer drugs. 7. 2-Guanidino-4-pyridylthiazoles as histamine H2-receptor antagonists with potent gastroprotective effects against nonsteroidal antiinflammatory drug-induced injury. | J Med Chem 37: 57-66 (1994) | Fujisawa Pharmaceutical Company, Ltd | 2D 3D TSV |
7903385 | 2 | Binding and functional characterization of alpha-2 adrenergic receptor subtypes on pig vascular endothelium. | J Pharmacol Exp Ther 267: 1126-33 (1993) | Creighton University | 2D 3D TSV |
7902871 | 35 | o-phenylphenols: potent and orally active leukotriene B4 receptor antagonists. | J Med Chem 36: 3978-81 (1993) | Eli Lilly and Company | 2D 3D TSV |
7902870 | 24 | Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors. | J Med Chem 36: 3929-36 (1994) | Warner-Lambert Company | 2D 3D TSV |
7902869 | 47 | N-(1-arylpropionyl)-4-aryltetrahydropyridines, a new class of high-affinity selective sigma receptor ligands. | J Med Chem 36: 3923-8 (1994) | New York University | 2D 3D TSV |
7902811 | 5 | Dopamine D1 receptors: efficacy of full (dihydrexidine) vs. partial (SKF38393) agonists in primates vs. rodents. | Eur J Pharmacol 242: 165-72 (1993) | University of North Carolina | 2D 3D TSV |
7902440 | 104 | Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins. | J Med Chem 36: 3556-64 (1994) | Hebrew University of Jerusalem | 2D 3D TSV |
7902439 | 31 | (R)-1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines: novel optically active compounds with strong 5-HT1A receptor binding ability exhibiting anticonflict activity and lessening of memory impairment. | J Med Chem 36: 3526-32 (1994) | Asahi Chemical Industry Company, Ltd. | 2D 3D TSV |
7901417 | 5 | Conformationally restricted analogues of remoxipride as potential antipsychotic agents. | J Med Chem 36: 3417-23 (1993) | Burroughs Wellcome Co. | 2D 3D TSV |
7901415 | 36 | Examination of the D2/5-HT2 affinity ratios of resolved 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: an enantioselective approach toward the design of potential atypical antipsychotics. | J Med Chem 36: 3073-6 (1993) | Scios Nova Inc | 2D 3D TSV |
7891350 | 9 | Pharmacologic characterization of CI-996, a new angiotensin receptor antagonist. | J Pharmacol Exp Ther 272: 963-9 (1995) | Parke-Davis Pharmaceutical Research | 2D 3D TSV |
7890738 | 3 | Expression of recombinant homo-oligomeric 5-hydroxytryptamine3 receptors provides new insights into their maturation and structure. | J Biol Chem 270: 6056-61 (1995) | Medical Research Council Centre | 2D 3D TSV |
7881740 | 3 | Mediation by 5-hydroxytryptamine2B receptors of endothelium-dependent relaxation in rat jugular vein. | Br J Pharmacol 114: 400-4 (1995) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7877140 | 74 | 2,4-Diamino-5-substituted-quinazolines as inhibitors of a human dihydrofolate reductase with a site-directed mutation at position 22 and of the dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii. | J Med Chem 38: 745-52 (1995) | Harvard Medical School | 2D 3D TSV |
7877139 | 8 | Orally bioavailable benzisothiazolone inhibitors of human leukocyte elastase. | J Med Chem 38: 739-44 (1995) | Sterling Winthrop Inc. | 2D 3D TSV |
7870182 | 115 | Molecular pharmacology of somatostatin receptors. | Naunyn Schmiedebergs Arch Pharmacol 350: 441-53 (1994) | Sandoz Pharma Ltd | 2D 3D TSV |
7862254 | 35 | Structural requirements for the occupancy of rat brain PACAP receptors and adenylate cyclase activation. | Neuropharmacology 33: 1189-95 (1994) | Université Libre de Bruxelles | 2D 3D TSV |
7861420 | 62 | C-9 and N-substituted analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3- propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A receptor agonists with various degrees of metabolic stability. | J Med Chem 38: 725-34 (1995) | Upjohn Laboratories | 2D 3D TSV |
7861418 | 61 | Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors. | J Med Chem 38: 708-14 (1995) | Vanderbilt University | 2D 3D TSV |
7861417 | 71 | Synthesis and structure-activity relationships of oxamic acid and acetic acid derivatives related to L-thyronine. | J Med Chem 38: 695-707 (1995) | CIBA Pharmaceuticals | 2D 3D TSV |
7861416 | 90 | Dual-acting thromboxane receptor antagonist/synthase inhibitors: synthesis and biological properties of [2-substituted-4-(3-pyridyl)-1,3-dioxan-5-yl] alkenoic acids. | J Med Chem 38: 686-94 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7861415 | 3 | Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma. | J Med Chem 38: 669-85 (1995) | Solvay Pharma | 2D 3D TSV |
7861414 | 36 | Three-dimensional quantitative structure-activity relationships of sulfonamide endothelin inhibitors. | J Med Chem 38: 659-68 (1995) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
7861413 | 11 | (R)-11-hydroxy- and (R)-11-hydroxy-10-methylaporphine: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions. | J Med Chem 38: 647-58 (1995) | Uppsala University | 2D 3D TSV |
7861405 | 9 | Highly kappa receptor-selective dynorphin A analogues with modifications in position 3 of dynorphin A(1-11)-NH2. | J Med Chem 38: 585-6 (1995) | University of Arizona | 2D 3D TSV |
7861404 | 29 | Inhibitors of HIV-1 protease containing the novel and potent (R)-(hydroxyethyl)sulfonamide isostere. | J Med Chem 38: 581-4 (1995) | Searle Discovery Research | 2D 3D TSV |
7855217 | 139 | Binding of antidepressants to human brain receptors: focus on newer generation compounds. | Psychopharmacology (Berl) 114: 559-65 (1994) | Mayo Clinic | 2D 3D TSV |
7855175 | 8 | PET examination of [11C]NNC 687 and [11C]NNC 756 as new radioligands for the D1-dopamine receptor. | Psychopharmacology (Berl) 113: 149-56 (1993) | Karolinska Institutet | 2D 3D TSV |
7853350 | 33 | Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol. | J Med Chem 38: 570-9 (1995) | University of Washington | 2D 3D TSV |
7853349 | 19 | (+)-cis-N-(para-, meta-, and ortho-substituted benzyl)-N-normetazocines: synthesis and binding affinity at the [3H]-(+)-pentazocine-labeled (sigma 1) site and quantitative structure-affinity relationship studies. | J Med Chem 38: 565-9 (1995) | Research Triangle Institute | 2D 3D TSV |
7853346 | 13 | Synthesis of novel thiol-containing citric acid analogues. Kinetic evaluation of these and other potential active-site-directed and mechanism-based inhibitors of ATP citrate lyase. | J Med Chem 38: 537-43 (1995) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7853341 | 115 | 3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships. | J Med Chem 38: 473-87 (1995) | Uppsala University | 2D 3D TSV |
7853337 | 12 | Cosalane analogues with enhanced potencies as inhibitors of HIV-1 protease and integrase. | J Med Chem 38: 443-52 (1995) | Purdue University | 2D 3D TSV |
7853336 | 6 | Phosphinyl acid-based bisubstrate analog inhibitors of Ras farnesyl protein transferase. | J Med Chem 38: 435-42 (1995) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
7853332 | 27 | 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice. | J Med Chem 38: 402-7 (1995) | University of Minnesota | 2D 3D TSV |
7853331 | 7 | Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. | J Med Chem 38: 395-401 (1995) | Glaxo Research Institute | 2D 3D TSV |
7853174 | 25 | In vivo receptor occupancy of the angiotensin II receptor by nonpeptide antagonists: relationship to in vitro affinities and in vivo pharmacologic potency. | J Pharmacol Exp Ther 272: 612-8 (1995) | Merck Research Laboratories | 2D 3D TSV |
7852999 | 6 | Cucurbitacins, Cell Adhesion Inhibitors from Conobea scoparioides | J Nat Prod 57: 1498-1502 (1994) | TBA | 2D 3D TSV |
7845473 | 3 | 5-Hydroxytryptamine receptors with a 5-HT6 receptor-like profile stimulating adenylyl cyclase activity in pig caudate membranes. | Naunyn Schmiedebergs Arch Pharmacol 350: 356-60 (1994) | Sandoz Pharma Ltd | 2D 3D TSV |
7837246 | 39 | Nonpeptidic inhibitors of human leukocyte elastase. 5. Design, synthesis, and X-ray crystallography of a series of orally active 5-aminopyrimidin-6-one-containing trifluoromethyl ketones. | J Med Chem 38: 98-108 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7837245 | 4 | Potent non-peptide fibrinogen receptor antagonists which present an alternative pharmacophore. | J Med Chem 38: 9-12 (1995) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7837244 | 33 | Non-peptidic inhibitors of human leukocyte elastase. 4. Design, synthesis, and in vitro and in vivo activity of a series of beta-carbolinone-containing trifluoromethyl ketones. | J Med Chem 38: 86-97 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7837243 | 25 | Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 2. Effect of varying the heterocyclic ring on in vitro potency. | J Med Chem 38: 76-85 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7837242 | 24 | Derivatives of 2-[[N-(Aminocarbonyl)-N-hydroxyamino]methyl]-1,4- benzodioxan as orally active 5-lipoxygenase inhibitors. | J Med Chem 38: 68-75 (1995) | Ciba-Geigy Corporation | 2D 3D TSV |
7837241 | 77 | Tyrosine kinase inhibitors. 4. Structure-activity relationships among N- and 3-substituted 2,2'-dithiobis(1H-indoles) for in vitro inhibition of receptor and nonreceptor protein tyrosine kinases. | J Med Chem 38: 58-67 (1995) | University of Auckland | 2D 3D TSV |
7837240 | 19 | Preparation of 18F-labeled muscarinic agonist with M2 selectivity. | J Med Chem 38: 5-8 (1995) | National Institutes of Health | 2D 3D TSV |
7837239 | 36 | Synthesis, properties, and pharmacokinetic studies of N2-phenylguanine derivatives as inhibitors of herpes simplex virus thymidine kinases. | J Med Chem 38: 49-57 (1995) | University of Massachusetts Medical School | 2D 3D TSV |
7837237 | 37 | Novel thiazole-based heterocycles as selective inhibitors of fibrinogen-mediated platelet aggregation. | J Med Chem 38: 34-41 (1995) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
7837236 | 19 | (+)-cis-4,5,7a,8,9,10,11,11a-octahydro-7H-10-methylindolo[1,7- bc][2,6]-naphthyridine: a 5-HT2C/2B receptor antagonist with low 5-HT2A receptor affinity. | J Med Chem 38: 28-33 (1995) | Sandoz Pharma Ltd. | 2D 3D TSV |
7837235 | 9 | Nonpeptidic inhibitors of human leukocyte elastase. 6. Design of a potent, intratracheally active, pyridone-based trifluoromethyl ketone. | J Med Chem 38: 212-5 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7837233 | 21 | CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623). | J Med Chem 38: 207-11 (1995) | Glaxo Research Institute | 2D 3D TSV |
7837225 | 40 | Ac-[3- and 4-alkylthioproline31]-CCK4 analogs: synthesis and implications for the CCK-B receptor-bound conformation. | J Med Chem 38: 137-49 (1995) | Washington University | 2D 3D TSV |
7837223 | 33 | Benzophenone- and indolecarboxylic acids: potent type-2 specific inhibitors of human steroid 5 alpha-reductase. | J Med Chem 38: 13-5 (1995) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7837222 | 14 | Calcium entry blockers and activators: conformational and structural determinants of dihydropyrimidine calcium channel modulators. | J Med Chem 38: 119-29 (1995) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
7837220 | 5 | Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. | J Med Chem 38: 1-4 (1995) | BioChem Therapeutic Inc. | 2D 3D TSV |
7830490 | 21 | SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor. | Life Sci 56: -32 (1995) | Sanofi Recherche | 2D 3D TSV |
7830281 | 237 | Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. | J Med Chem 38: 379-88 (1995) | Research Triangle Institute | 2D 3D TSV |
7830274 | 22 | Evaluation of cis- and trans-9- and 11-hydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridines as structurally rigid, selective D1 dopamine receptor ligands. | J Med Chem 38: 318-27 (1995) | Purdue University | 2D 3D TSV |
7830273 | 49 | A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site. | J Med Chem 38: 305-17 (1995) | Merck Research Laboratories | 2D 3D TSV |
7830269 | 9 | Homologs of histamine as histamine H3 receptor antagonists: a new potent and selective H3 antagonist, 4(5)-(5-aminopentyl)-1H-imidazole. | J Med Chem 38: 266-71 (1995) | Vrije Universiteit Amsterdam | 2D 3D TSV |
7830265 | 34 | Antitumor activity of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinolines. | J Med Chem 38: 234-40 (1995) | Sandoz Research Institute | 2D 3D TSV |
7830264 | 16 | Inhibition of human neutrophil elastase. 3. An orally active enol acetate prodrug. | J Med Chem 38: 223-33 (1995) | Marion Merrell Dow Research Institute | 2D 3D TSV |
7815359 | 29 | Characterization of the cloned human mu opioid receptor. | J Pharmacol Exp Ther 272: 423-8 (1995) | University of Pennsylvania | 2D 3D TSV |
7815325 | 65 | Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. | J Pharmacol Exp Ther 272: 134-42 (1995) | Duke University | 2D 3D TSV |
7807122 | 4 | New cytotoxic peroxylactones from the marine sponge, Plakinastrella onkodes. | J Nat Prod 57: 1374-81 (1994) | Harbor Branch Oceanographic Institution, Inc. | 2D 3D TSV |
7807119 | 5 | Khusimol, a Non-Peptide Ligand for Vasopressin V1a Receptors | J Nat Prod 57: 1329-1335 (1994) | TBA | 2D 3D TSV |
7805774 | 9 | Binding profile of the selective muscarinic receptor antagonist tripitramine. | Eur J Pharmacol 268: 459-62 (1994) | University of Pisa | 2D 3D TSV |
7805764 | 11 | The pharmacological profile of cloned and stably expressed alpha 1b-adrenoceptor in CHO cells. | Eur J Pharmacol 268: 399-407 (1994) | National Children's Medical Research Center | 2D 3D TSV |
7799410 | 46 | Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. | J Med Chem 37: 4576-80 (1995) | Heidelberg | 2D 3D TSV |
7799409 | 20 | Derivatives of 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pyridinyl-p-iodobenzamido)ethyl]pipera zine (p-MPPI) as 5-HT1A ligands. | J Med Chem 37: 4572-5 (1995) | University of Pennsylvania | 2D 3D TSV |
7799404 | 22 | Inhibition of human neutrophil elastase with peptidyl electrophilic ketones. 2. Orally active PG-Val-Pro-Val pentafluoroethyl ketones. | J Med Chem 37: 4538-53 (1995) | Marion Merrell Dow Research Institute | 2D 3D TSV |
7799402 | 42 | 2,4-Diamino-5-chloroquinazoline analogues of trimetrexate and piritrexim: synthesis and antifolate activity. | J Med Chem 37: 4522-8 (1995) | Institute | 2D 3D TSV |
7799400 | 5 | A conformationally defined 6-s-trans-retinoic acid isomer: synthesis, chemopreventive activity, and toxicity. | J Med Chem 37: 4499-507 (1995) | University of Alabama at Birmingham | 2D 3D TSV |
7799399 | 8 | kappa Opioid receptor selective affinity labels: electrophilic benzeneacetamides as kappa-selective opioid antagonists. | J Med Chem 37: 4490-8 (1995) | University of Minnesota | 2D 3D TSV |
7799398 | 5 | The discovery of novel, structurally diverse protein kinase C agonists through computer 3D-database pharmacophore search. Molecular modeling studies. | J Med Chem 37: 4479-89 (1995) | National Cancer Institute-Bethesda | 2D 3D TSV |
7799397 | 86 | Triazolinone biphenylsulfonamides as angiotensin II receptor antagonists with high affinity for both the AT1 and AT2 subtypes. | J Med Chem 37: 4464-78 (1995) | Merck Research Laboratories | 2D 3D TSV |
7796807 | 51 | The 5-HT4 receptor: molecular cloning and pharmacological characterization of two splice variants. | EMBO J 14: 2806-15 (1995) | Synaptic Pharmaceutical Corporation | 2D 3D TSV |
7791120 | 11 | Characterization and distribution of binding sites for a new neurotensin receptor antagonist ligand, [3H]SR 48692, in the guinea pig brain. | J Pharmacol Exp Ther 273: 1450-8 (1995) | Hospital Saint-Antoine | 2D 3D TSV |
7791071 | 20 | RP 73870, a gastrin/cholecystokinin-B receptor antagonist with potent anti-ulcer activity in the rat. | J Pharmacol Exp Ther 273: 1015-22 (1995) | Rhone-Poulenc Rorer Central Research | 2D 3D TSV |
7783157 | 14 | 2-Phenyl-4-(aminomethyl)imidazoles as potential antipsychotic agents. Synthesis and dopamine D2 receptor binding. | J Med Chem 38: 2251-5 (1995) | Neurogen Corporation | 2D 3D TSV |
7783156 | 35 | New analogs of burimamide as potent and selective histamine H3 receptor antagonists: the effect of chain length variation of the alkyl spacer and modifications of the N-thiourea substituent. | J Med Chem 38: 2244-50 (1995) | Vrije Universiteit Amsterdam | 2D 3D TSV |
7783155 | 10 | Identification of 3,5-dihydro-2-aryl-1H-pyrazolo[3,4-c]quinoline-1,4(2H)-diones as novel high-affinity glycine site N-methyl-D-aspartate antagonists. | J Med Chem 38: 2239-43 (1995) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
7783153 | 189 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 2. Effects of 8-amino nitrogen substitution on serotonin receptor binding and pharmacology. | J Med Chem 38: 2217-30 (1995) | Upjohn Laboratories | 2D 3D TSV |
7783152 | 170 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. | J Med Chem 38: 2202-16 (1995) | Göteborg University | 2D 3D TSV |
7783150 | 33 | Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors. | J Med Chem 38: 2188-95 (1995) | Royal Danish School of Pharmacy | 2D 3D TSV |
7783147 | 39 | Novel 2,4-diamino-5-substituted-pyrrolo[2,3-d]pyrimidines as classical and nonclassical antifolate inhibitors of dihydrofolate reductases. | J Med Chem 38: 2158-65 (1995) | Duquesne University | 2D 3D TSV |
7783144 | 10 | Development of a novel series of trialkoxyaryl derivatives as specific and competitive antagonists of platelet activating factor. | J Med Chem 38: 2130-7 (1995) | Wellcome Research Laboratories | 2D 3D TSV |
7783143 | 66 | Hydroxamic acids as potent inhibitors of endothelin-converting enzyme from human bronchiolar smooth muscle. | J Med Chem 38: 2119-29 (1995) | Berlex Laboratories | 2D 3D TSV |
7783141 | 28 | Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom. | J Med Chem 38: 2103-11 (1995) | Universität des Saarlandes | 2D 3D TSV |
7783140 | 47 | Receptor surface models. 2. Application to quantitative structure-activity relationships studies. | J Med Chem 38: 2091-102 (1995) | Molecular Simulations Inc | 2D 3D TSV |
7783136 | 35 | Design and synthesis of new naphthalenic derivatives as ligands for 2-[125I]iodomelatonin binding sites. | J Med Chem 38: 2050-60 (1995) | CNRS-BIOCIS | 2D 3D TSV |
7783135 | 20 | Synthesis, antitubulin and antimitotic activity, and cytotoxicity of analogs of 2-methoxyestradiol, an endogenous mammalian metabolite of estradiol that inhibits tubulin polymerization by binding to the colchicine binding site. | J Med Chem 38: 2041-9 (1995) | Purdue University | 2D 3D TSV |
7783132 | 82 | Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines. | J Med Chem 38: 2009-17 (1995) | H. Lundbeck A/S | 2D 3D TSV |
7783131 | 78 | Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. | J Med Chem 38: 1998-2008 (1995) | H. Lundbeck A/S | 2D 3D TSV |
7783126 | 29 | N4-unsubstituted N1-arylpiperazines as high-affinity 5-HT1A receptor ligands. | J Med Chem 38: 1942-54 (1995) | Solvay Duphar Research Laboratories | 2D 3D TSV |
7783121 | 20 | Synthesis and biological evaluation of novel 2,6-diaminobenz[cd]indole inhibitors of thymidylate synthase using the protein structure as a guide. | J Med Chem 38: 1892-903 (1995) | Agouron Pharmaceuticals Inc | 2D 3D TSV |
7783120 | 12 | Use of medium-sized cycloalkyl rings to enhance secondary binding: discovery of a new class of human immunodeficiency virus (HIV) protease inhibitors. | J Med Chem 38: 1884-91 (1995) | Upjohn | 2D 3D TSV |
7783119 | 7 | Carbethoxylating agents as inhibitors of aldehyde dehydrogenase. | J Med Chem 38: 1872-6 (1995) | University of Minnesota | 2D 3D TSV |
7783118 | 3 | Prodrugs of nitroxyl as potential aldehyde dehydrogenase inhibitors vis-a-vis vascular smooth muscle relaxants. | J Med Chem 38: 1865-71 (1995) | University of Minnesota | 2D 3D TSV |
7783114 | 21 | Design and syntheses of potent and selective dipeptide inhibitors of Candida albicans myristoyl-CoA:protein N-myristoyltransferase. | J Med Chem 38: 1837-40 (1995) | G.D. Searle and Co. | 2D 3D TSV |
7774675 | 35 | Characterisation of melanocortin receptor subtypes by radioligand binding analysis. | Eur J Pharmacol 288: 311-7 (1995) | Uppsala | 2D 3D TSV |
7774670 | 11 | Pharmacological properties of two recombinant splice variants of the PACAP type I receptor, transfected and stably expressed in CHO cells. | Eur J Pharmacol 288: 259-67 (1995) | Université Libre de Bruxelles | 2D 3D TSV |
7769390 | 7 | Flavonoids as DNA topoisomerase antagonists and poisons: structure-activity relationships. | J Nat Prod 58: 217-25 (1995) | University of Illinois at Chicago | 2D 3D TSV |
7754369 | 4 | Identification and characterization of a prostaglandin transporter. | Science 268: 866-869 (1995) | Albert Einstein College of Medicine | 2D 3D TSV |
7752206 | 20 | Inhibition of herpes simplex virus type 1 helicase-primase by (dichloroanilino)purines and -pyrimidines. | J Med Chem 38: 1820-5 (1995) | Stanford University Medical School | 2D 3D TSV |
7752204 | 98 | Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors. | J Med Chem 38: 1799-810 (1995) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
7752201 | 68 | 6-substituted 2,4-diamino-5-methylpyrido[2,3-d]pyrimidines as inhibitors of dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents. | J Med Chem 38: 1778-85 (1995) | Duquesne University | 2D 3D TSV |
7752200 | 8 | S-(5'-deoxy-5'-adenosyl)-1-aminoxy-4-(methylsulfonio)-2-cyclopentene (AdoMao): an irreversible inhibitor of S-adenosylmethionine decarboxylase with potent in vitro antitrypanosomal activity. | J Med Chem 38: 1770-7 (1995) | Wayne State University | 2D 3D TSV |
7752199 | 71 | Effects of a D-Cys6/L-Cys6 interchange in nonselective and selective vasopressin and oxytocin antagonists. | J Med Chem 38: 1762-9 (1995) | Medical College of Ohio | 2D 3D TSV |
7752198 | 8 | Time-resolved ligand exchange reactions: kinetic models for competitive inhibitors with recombinant human renin. | J Med Chem 38: 1751-61 (1995) | Boehringer Ingelheim Pharmaceuticals Inc | 2D 3D TSV |
7752196 | 103 | Structure-activity relationships of 9-alkyladenine and ribose-modified adenosine derivatives at rat A3 adenosine receptors. | J Med Chem 38: 1720-35 (1995) | National Institute of Diabetes | 2D 3D TSV |
7752195 | 30 | Syntheses and biological properties of chiral fluoroalkyl quinuclidinyl benzilates. | J Med Chem 38: 1711-9 (1995) | National Institutes of Health | 2D 3D TSV |
7752194 | 5 | Buspirone analogues as ligands of the 5-HT1A receptor. 1. The molecular structure of buspirone and its two analogues. | J Med Chem 38: 1701-10 (1995) | Pharmaceutical Research Institute | 2D 3D TSV |
7752193 | 43 | Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. | J Med Chem 38: 1689-700 (1995) | Ciba-Geigy Corporation | 2D 3D TSV |
7752186 | 29 | A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors. | J Med Chem 38: 1608-28 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7752185 | 34 | Substituted (1,2-diarylethyl)amide acyl-CoA:cholesterol acyltransferase inhibitors: effect of polar groups on in vitro and in vivo activity. | J Med Chem 38: 1600-7 (1995) | Schering-Plough Research Institute | 2D 3D TSV |
7752184 | 12 | A novel pyrrolidine analog of histamine as a potent, highly selective histamine H3 receptor agonist. | J Med Chem 38: 1593-9 (1995) | Schering-Plough Research Institute | 2D 3D TSV |
7752183 | 22 | Design and evaluation of nonpeptide fibrinogen gamma-chain based GPIIb/IIIa antagonists. | J Med Chem 38: 1582-92 (1995) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
7752182 | 41 | Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine. | J Med Chem 38: 1579-81 (1995) | Synaptic Pharmaceutical Corporation | 2D 3D TSV |
7751958 | 23 | Molecular, functional, and pharmacological characterization of the metabotropic glutamate receptor type 5 splice variants: comparison with mGluR1. | J Neurosci 15: 3970-81 (1995) | CNRS CCIPE | 2D 3D TSV |
7739015 | 12 | Phosphonates and phosphinates: novel leaving groups for benzisothiazolone inhibitors of human leukocyte elastase. | J Med Chem 38: 1571-4 (1995) | Sterling Winthrop Pharmaceuticals Research Division | 2D 3D TSV |
7739014 | 23 | In vitro muscarinic activity of spiromuscarones and related analogs. | J Med Chem 38: 1558-70 (1995) | Fisons Pharmaceuticals | 2D 3D TSV |
7739013 | 26 | Enantiomers of diastereomeric cis-N-[1-(2-hydroxy-2-phenylethyl)- 3-methyl-4-piperidyl]-N-phenylpropanamides: synthesis, X-ray analysis, and biological activities. | J Med Chem 38: 1547-57 (1995) | Research Triangle Institute | 2D 3D TSV |
7739011 | 90 | Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands. | J Med Chem 38: 1523-37 (1995) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
7739010 | 118 | Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. | J Med Chem 38: 1511-22 (1995) | Thrombosis Research Institute | 2D 3D TSV |
7739009 | 34 | Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines. | J Med Chem 38: 1505-10 (1995) | Glaxo Research Institute | 2D 3D TSV |
7739006 | 2 | Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds. | J Med Chem 38: 1473-81 (1995) | Wyeth Research (U.K.) Ltd. | 2D 3D TSV |
7739005 | 143 | 2-Aralkynyl and 2-heteroalkynyl derivatives of adenosine-5'-N-ethyluronamide as selective A2a adenosine receptor agonists. | J Med Chem 38: 1462-72 (1995) | Universit£ di Camerino | 2D 3D TSV |
7739004 | 12 | Synthesis and in vitro evaluation of 4-substituted N-(1,1-dimethylethyl)-3-oxo-4-androstene-17 beta-carboxamides as 5 alpha-reductase inhibitors and antiandrogens. | J Med Chem 38: 1456-61 (1995) | CHUL Research Center | 2D 3D TSV |
7738999 | 88 | Metabotropic glutamate receptors: novel targets for drug development. | J Med Chem 38: 1417-26 (1995) | CNS Research | 2D 3D TSV |
7731020 | 87 | Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists. | J Med Chem 38: 1344-54 (1995) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
7731019 | 16 | Electrophilic N-benzylnaltrindoles as delta opioid receptor-selective antagonists. | J Med Chem 38: 1337-43 (1995) | University of Minnesota | 2D 3D TSV |
7731018 | 64 | Tricyclic heteroaromatic systems. Synthesis and A1 and A2a adenosine binding activities of some 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c] pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]quinolin-4- ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines. | J Med Chem 38: 1330-6 (1995) | Università di Firenze | 2D 3D TSV |
7731017 | 46 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of monopropyl analogs of 5-, 7-, and 8-[[(trifluoromethyl)sulfonyl]oxy]-2-aminotetralins: central dopamine and serotonin receptor activity. | J Med Chem 38: 1319-29 (1995) | University of G£teborg | 2D 3D TSV |
7731016 | 55 | Quantitative binding site model generation: compass applied to multiple chemotypes targeting the 5-HT1A receptor. | J Med Chem 38: 1295-308 (1995) | Arris Pharmaceutical Corporation | 2D 3D TSV |
7731015 | 15 | Synthesis and histamine H1 receptor agonist activity of a series of 2-phenylhistamines, 2-heteroarylhistamines, and analogues. | J Med Chem 38: 1287-94 (1995) | Freie Universit£t Berlin | 2D 3D TSV |
7731013 | 32 | New (2-methoxyphenyl)piperazine derivatives as 5-HT1A receptor ligands with reduced alpha 1-adrenergic activity. Synthesis and structure-affinity relationships. | J Med Chem 38: 1273-7 (1995) | FAES, S.A. | 2D 3D TSV |
7731012 | 5 | Farnesyl derivatives of rigid carboxylic acids-inhibitors of ras-dependent cell growth. | J Med Chem 38: 1267-72 (1995) | Institute for Biological Research | 2D 3D TSV |
7731011 | 5 | 4,4-Disubstituted piperidines: a new class of NK1 antagonist. | J Med Chem 38: 1264-6 (1995) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
7731010 | 56 | Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists. | J Med Chem 38: 1259-63 (1995) | Warner-Lambert Company | 2D 3D TSV |
7724556 | 15 | Protein structure-based design of potent orally bioavailable, nonpeptide inhibitors of human immunodeficiency virus protease. | Proc Natl Acad Sci U S A 92: 3298-302 (1995) | Agouron Pharmaceuticals Inc | 2D 3D TSV |
7716273 | 19 | Properties of the VIP-PACAP type II receptor stably expressed in CHO cells. | Regul Pept 54: 397-407 (1994) | Université Libre de Bruxelles | 2D 3D TSV |
7714543 | 1 | Ophirapstanol trisulfate, a new biologically active steroid sulfate from the deep water marine sponge Topsentia ophiraphidites. | J Nat Prod 57: 1751-4 (1994) | Harbor Branch Oceanographic Institution, Inc. | 2D 3D TSV |
7707326 | 39 | Opioid receptor binding requirements for the delta-selective peptide deltorphin. I: Phe3 replacement with ring-substituted and heterocyclic amino acids. | J Med Chem 38: 1242-6 (1995) | Eastern Michigan University | 2D 3D TSV |
7707324 | 22 | Synthesis of alkyl chain-modified ether lipids and evaluation of their in vitro cytotoxicity. | J Med Chem 38: 1216-28 (1995) | Laboratorios Menarini S.A. | 2D 3D TSV |
7707322 | 52 | Ketanserin analogues: the effect of structural modification on 5-HT2 serotonin receptor binding. | J Med Chem 38: 1196-202 (1995) | Virginia Commonwealth University | 2D 3D TSV |
7707320 | 99 | Search for new purine- and ribose-modified adenosine analogues as selective agonists and antagonists at adenosine receptors. | J Med Chem 38: 1174-88 (1995) | National Institute of Diabetes | 2D 3D TSV |
7707319 | 81 | Synthesis and in vitro activity of 17 beta-(N-alkyl/arylformamido)- and 17 beta-[(N-alkyl/aryl)alkyl/arylamido]-4-methyl-4-aza-3-oxo-5 alpha-androstan-3-ones as inhibitors of human 5 alpha-reductases and antagonists of the androgen receptor. | J Med Chem 38: 1158-73 (1995) | CHUL Research Center | 2D 3D TSV |
7707318 | 19 | Novel modified carboxy terminal fragments of neuropeptide Y with high affinity for Y2-type receptors and potent functional antagonism at a Y1-type receptor. | J Med Chem 38: 1150-7 (1995) | Burroughs Wellcome Company | 2D 3D TSV |
7707316 | 32 | Mapping the melatonin receptor. 3. Design and synthesis of melatonin agonists and antagonists derived from 2-phenyltryptamines. | J Med Chem 38: 1132-9 (1995) | University College London | 2D 3D TSV |
7707315 | 58 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). | J Med Chem 38: 1119-31 (1995) | Hoechst-Roussel Pharmaceuticals Inc | 2D 3D TSV |
7707314 | 23 | Synthesis, topoisomerase I inhibitory activity, and in vivo evaluation of 11-azacamptothecin analogs. | J Med Chem 38: 1106-18 (1995) | Glaxo Inc. Research Institute | 2D 3D TSV |
7707311 | 18 | Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors. | J Med Chem 38: 1084-9 (1995) | Pfizer Inc | 2D 3D TSV |
7707310 | 51 | Design, synthesis, and structure--activity relationship studies for a new imidazole series of J774 macrophage specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors. | J Med Chem 38: 1067-83 (1995) | DuPont Pharmaceuticals Company | 2D 3D TSV |
7707308 | 3 | Novel thiazole based heterocycles as inhibitors of LFA-1/ICAM-1 mediated cell adhesion. | J Med Chem 38: 1057-9 (1995) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
7705353 | 24 | Thermodynamics of antigen-antibody binding using specific anti-lysozyme antibodies. | Eur J Biochem 228: 388-94 (1995) | University of Maryland Biotechnology Institute | 2D 3D TSV |
7699716 | 41 | Quinazoline antifolate thymidylate synthase inhibitors: replacement of glutamic acid in the C2-methyl series. | J Med Chem 38: 994-1004 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7699713 | 76 | Quantitative structure-activity relationships of the inhibition of Pneumocystis carinii dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(X-phenyl)-s-triazines. | J Med Chem 38: 967-72 (1995) | COR Therapeutics Inc | 2D 3D TSV |
7699712 | 20 | Stereoselective LSD-like activity in a series of d-lysergic acid amides of (R)- and (S)-2-aminoalkanes. | J Med Chem 38: 958-66 (1995) | Purdue University | 2D 3D TSV |
7699710 | 84 | High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2. | J Med Chem 38: 942-9 (1995) | Università di Bari | 2D 3D TSV |
7699709 | 22 | Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage. | J Med Chem 38: 923-33 (1995) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
7699707 | 7 | Dicationic diarylfurans as anti-Pneumocystis carinii agents. | J Med Chem 38: 912-6 (1995) | Georgia State University | 2D 3D TSV |
7699706 | 34 | Rigid analogs of camptothecin as DNA topoisomerase I inhibitors. | J Med Chem 38: 906-11 (1995) | Glaxo Research Institute | 2D 3D TSV |
7699705 | 19 | Nonpeptidic potent HIV-1 protease inhibitors: (4-hydroxy-6-phenyl-2-oxo-2H- pyran-3-yl)thiomethanes that span P1-P2' subsites in a unique mode of active site binding. | J Med Chem 38: 898-905 (1995) | Parke-Davis Pharmaceutical Research | 2D 3D TSV |
7699704 | 30 | Three-dimensional quantitative structure-activity relationship (QSAR) of HIV integrase inhibitors: a comparative molecular field analysis (CoMFA) study. | J Med Chem 38: 890-7 (1995) | National Cancer Institute-Bethesda | 2D 3D TSV |
7699700 | 23 | Second-generation leukotriene B4 receptor antagonists related to SC-41930: heterocyclic replacement of the methyl ketone pharmacophore. | J Med Chem 38: 858-68 (1995) | Searle Research and Development | 2D 3D TSV |
7699699 | 5 | N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT2B receptor antagonist. | J Med Chem 38: 855-7 (1995) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7699697 | 34 | Acylshikonin analogues: synthesis and inhibition of DNA topoisomerase-I. | J Med Chem 38: 1044-7 (1995) | Chungnam National University | 2D 3D TSV |
7699694 | 66 | Synthesis and biological activity of 7-alkylidenecephems. | J Med Chem 38: 1022-34 (1995) | Southern Methodist University | 2D 3D TSV |
7699693 | 13 | Ketomethylene and (cyanomethylene)amino pseudopeptide analogues of the C-terminal hexapeptide of neurotensin. | J Med Chem 38: 1015-21 (1995) | Instituto de Qu£mica M£dica (CSIC) | 2D 3D TSV |
7699692 | 14 | [[(Guaninylalkyl)phosphinico]methyl]phosphonic acids. Multisubstrate analogue inhibitors of human erythrocyte purine nucleoside phosphorylase. | J Med Chem 38: 1005-14 (1995) | Burroughs Wellcome Co. | 2D 3D TSV |
7695269 | 20 | Inhibition of cap (m7GpppXm)-dependent endonuclease of influenza virus by 4-substituted 2,4-dioxobutanoic acid compounds. | Antimicrob Agents Chemother 38: 2827-37 (1995) | Merck Research Laboratories | 2D 3D TSV |
7693945 | 6 | Synthesis, in vitro binding profile, and autoradiographic analysis of [3H]-cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine, a highly potent and selective nonpeptide substance P receptor antagonist radioligand. | J Med Chem 36: 3197-201 (1993) | Pfizer Inc | 2D 3D TSV |
7693944 | 51 | 14 beta-[(p-nitrocinnamoyl)amino]morphinones, 14 beta-[(p-nitrocinnamoyl)amino]-7,8-dihydromorphinones, and their codeinone analogues: synthesis and receptor activity. | J Med Chem 36: 3154-60 (1993) | Institute | 2D 3D TSV |
7692048 | 48 | Synthesis and biological evaluation of cholecystokinin analogs in which the Asp-Phe-NH2 moiety has been replaced by a 3-amino-7-phenylheptanoic acid or a 3-amino-6-(phenyloxy)hexanoic acid. | J Med Chem 36: 3021-8 (1993) | EP CNRS 51 | 2D 3D TSV |
7689652 | 6 | Studies on neurokinin antagonists. 3. Design and structure-activity relationships of new branched tripeptides N alpha-(substituted L-aspartyl, L-ornithyl, or L-lysyl)-N-methyl-N-(phenylmethyl)-L-phenylalaninamides as substance P antagonists. | J Med Chem 36: 2266-78 (1993) | Fujisawa Pharmaceutical Co., Ltd | 2D 3D TSV |
7689109 | 83 | Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity. | J Med Chem 36: 2526-35 (1993) | Boehringer Mannheim GmbH | 2D 3D TSV |
7684452 | 66 | Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and"mixed" CCK-A/CCK-B antagonists. | J Med Chem 36: 552-65 (1993) | Parke-Davis Neuroscience Research Centre | 2D 3D TSV |
7684450 | 26 | Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a | J Med Chem 36: 1505-8 (1993) | Upjohn | 2D 3D TSV |
7683725 | 30 | 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. | J Med Chem 36: 1291-4 (1993) | Merck Research Laboratories | 2D 3D TSV |
7683054 | 115 | Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogues. | J Med Chem 36: 953-66 (1993) | Merck Reserch Laboratories | 2D 3D TSV |
7682702 | 31 | Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain. | Proc Natl Acad Sci U S A 90: 3452-6 (1993) | The Scripps Research Institute | 2D 3D TSV |
7681480 | 7 | Non-nucleoside inhibitors of HIV-1 reverse transcriptase: molecular modeling and X-ray structure investigations. | J Med Chem 36: 726-32 (1993) | Boehringer Mannheim GmbH | 2D 3D TSV |
7681406 | 8 | Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors. | Eur J Pharmacol 232: 13-9 (1993) | Sanofi Recherche | 2D 3D TSV |
7680751 | 48 | Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. | Mol Pharmacol 43: 320-7 (1993) | National Institute of Neurological Disorders and Stroke | 2D 3D TSV |
7678654 | 30 | Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one. | J Med Chem 36: 249-55 (1993) | Merck Research Laboratories | 2D 3D TSV |
7678430 | 23 | Cyclic peptides as selective tachykinin antagonists. | J Med Chem 36: 2-10 (1993) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
7673944 | 1 | Bis(sulfato)-cyclosiphonodictyol A, a new disulfated sesquiterpene-hydroquinone from a deep water collection of the Marine sponge Siphonodictyon coralliphagum. | J Nat Prod 58: 958-60 (1995) | Harbor Branch Oceanographic Institution, Inc. | 2D 3D TSV |
7673943 | 1 | Aplysillin A, a Thrombin Receptor Antagonist from the Marine Sponge Aplysina fistularis fulva | J Nat Prod 58: 954-957 (1995) | TBA | 2D 3D TSV |
7673929 | 5 | Acetylcholinesterase inhibition by territrem B derivatives. | J Nat Prod 58: 857-862 (1995) | TBA | 2D 3D TSV |
7673927 | 6 | Isolation and Structure of Two Novel Muscarinic Receptor Antagonists | J Nat Prod 58: 843-847 (1995) | TBA | 2D 3D TSV |
7673925 | 3 | Flavonoid Inhibitors of Trypsin and Leucine Aminopeptidase: A Proposed Mathematical Model for IC50 Estimation | J Nat Prod 58: 823-829 (1995) | TBA | 2D 3D TSV |
7673199 | 4 | The affinity maturation of anti-4-hydroxy-3-nitrophenylacetyl mouse monoclonal antibody. A calorimetric study of the antigen-antibody interaction. | J Biol Chem 270: 22218-22 (1995) | Institute of Physical and Chemical Research (RIKEN) | 2D 3D TSV |
7664823 | 5 | Modulation of [35S]TBPS binding by ligands with preferential affinity for benzodiazepine BZ1 sites in the cerebral cortex of newborn and adult rats. | Eur J Pharmacol 290: 37-47 (1995) | University of Cagliari | 2D 3D TSV |
7658455 | 43 | Decapeptide agonists of human C5a: the relationship between conformation and neutrophil response. | J Med Chem 38: 3669-75 (1995) | University of Nebraska Medical Center | 2D 3D TSV |
7658454 | 65 | Nonclassical 2,4-diamino-6-(aminomethyl)-5,6,7,8-tetrahydroquinazoline antifolates: synthesis and biological activities. | J Med Chem 38: 3660-8 (1995) | Duquesne University | 2D 3D TSV |
7658453 | 16 | Stereoisomers of N-[1-hydroxy-(2-phenylethyl)-3-methyl-4-piperidyl]- N-phenylpropanamide: synthesis, stereochemistry, analgesic activity, and opioid receptor binding characteristics. | J Med Chem 38: 3652-9 (1995) | Institute of Materia Medica | 2D 3D TSV |
7658452 | 52 | Synthesis and evaluation of 5-amino-5,6,7,8-tetrahydroquinolinones as potential agents for the treatment of Alzheimer's disease. | J Med Chem 38: 3645-51 (1995) | Hoechst-Roussel Pharmaceuticals Inc | 2D 3D TSV |
7658450 | 20 | Structure-based design of novel HIV protease inhibitors: carboxamide-containing 4-hydroxycoumarins and 4-hydroxy-2-pyrones as potent nonpeptidic inhibitors. | J Med Chem 38: 3624-37 (1995) | Upjohn | 2D 3D TSV |
7658449 | 39 | Peptidomimetic inhibitors of herpes simplex virus ribonucleotide reductase: a new class of antiviral agents. | J Med Chem 38: 3617-23 (1995) | Bio-M£ga/Boehringer Ingelheim Research Inc. | 2D 3D TSV |
7658448 | 65 | Selective inhibitors of Candida albicans dihydrofolate reductase: activity and selectivity of 5-(arylthio)-2,4-diaminoquinazolines. | J Med Chem 38: 3608-16 (1995) | Burroughs Wellcome Company | 2D 3D TSV |
7658447 | 72 | Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors. | J Med Chem 38: 3602-7 (1995) | Centre de Recherche Pierre Fabre | 2D 3D TSV |
7658446 | 4 | Effect of a chiral 4-alkyl substituent in hallucinogenic amphetamines. | J Med Chem 38: 3593-601 (1995) | Purdue University | 2D 3D TSV |
7658444 | 56 | 2-[N'-(3-arylallylidene)hydrazino]adenosines showing A2a adenosine agonist properties and vasodilation activity. | J Med Chem 38: 3581-5 (1995) | Universit£ di Milano | 2D 3D TSV |
7658443 | 5 | Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties. | J Med Chem 38: 3566-80 (1995) | Wellcome Research Laboratories | 2D 3D TSV |
7658441 | 89 | Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities. | J Med Chem 38: 3547-57 (1995) | Biofor Inc. | 2D 3D TSV |
7658440 | 16 | Synthesis and quantitative structure-activity relationships of dequalinium analogues as K+ channel blockers: investigation into the role of the substituent at position 4 of the quinoline ring. | J Med Chem 38: 3536-46 (1995) | University College London | 2D 3D TSV |
7658439 | 43 | Novel antagonists of platelet-activating factor. 2. Synthesis and structure-activity relationships of potent and long-acting heterofused [1,5]benzodiazepine and [1,4]diazepine derivatives of 2-methyl-1-phenylimidazo[4,5-c]pyridine. | J Med Chem 38: 3524-35 (1995) | Pfizer Inc | 2D 3D TSV |
7658438 | 22 | Novel antagonists of platelet-activating factor. 1. Synthesis and structure-activity relationships of benzodiazepine and benzazepine derivatives of 2-methyl-1-phenylimidazo[4,5-c]pyridine. | J Med Chem 38: 3514-23 (1995) | Pfizer Inc | 2D 3D TSV |
7658437 | 25 | The squalestatins: synthesis and biological activity of some C3-modified analogues; replacement of a carboxylic acid or methyl ester with an isoelectronic heterocyclic functionality. | J Med Chem 38: 3502-13 (1995) | Glaxo Research and Development Ltd. | 2D 3D TSV |
7658435 | 49 | Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor. | J Med Chem 38: 3482-7 (1995) | University of Auckland | 2D 3D TSV |
7658434 | 52 | Functionally selective M1 muscarinic agonists. 3. Side chains and azacycles contributing to functional muscarinic selectivity among pyrazinylazacycles. | J Med Chem 38: 3469-81 (1995) | Eli Lilly and Company | 2D 3D TSV |
7658433 | 27 | Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1. | J Med Chem 38: 3462-8 (1995) | University of Arizona | 2D 3D TSV |
7658432 | 46 | Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. | J Med Chem 38: 3454-61 (1995) | University of Arizona | 2D 3D TSV |
7658431 | 18 | Synthesis and ligand binding study of 3 beta-(4'-substituted phenyl)-2 beta-(heterocyclic)tropanes. | J Med Chem 38: 3451-3 (1995) | Research Triangle Institute | 2D 3D TSV |
7658430 | 1 | Antidiabetic agents: a new class of reversible carnitine palmitoyltransferase I inhibitors. | J Med Chem 38: 3448-50 (1995) | Sandoz Research Institute | 2D 3D TSV |
7658429 | 31 | (5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431). | J Med Chem 38: 3445-7 (1995) | Abbott Laboratories | 2D 3D TSV |
7658428 | 94 | Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. | J Med Chem 38: 3415-44 (1995) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7651361 | 32 | Characterization of (+/-)(-)[3H]epibatidine binding to nicotinic cholinergic receptors in rat and human brain. | Mol Pharmacol 48: 280-7 (1995) | Georgetown University | 2D 3D TSV |
7650691 | 14 | Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands. | J Med Chem 38: 3384-90 (1995) | Glaxo Research Institute | 2D 3D TSV |
7650690 | 64 | Conformational effects on retinoid receptor selectivity. 2. Effects of retinoid bridging group on retinoid X receptor activity and selectivity. | J Med Chem 38: 3368-83 (1995) | SRI International | 2D 3D TSV |
7650689 | 12 | The role of water molecules in the structure-based design of (5-hydroxynorvaline)-2-cyclosporin: synthesis, biological activity, and crystallographic analysis with cyclophilin A. | J Med Chem 38: 3361-7 (1995) | Sandoz Pharma Ltd | 2D 3D TSV |
7650688 | 6 | The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor. | J Med Chem 38: 3351-60 (1995) | Vrije Universiteit | 2D 3D TSV |
7650687 | 22 | Design of potent non-thiourea H3-receptor histamine antagonists. | J Med Chem 38: 3342-50 (1995) | University College London | 2D 3D TSV |
7650686 | 3 | Non-peptide fibrinogen receptor antagonists. 7. Design and synthesis of a potent, orally active fibrinogen receptor antagonist. | J Med Chem 38: 3332-41 (1995) | Merck Research Laboratories | 2D 3D TSV |
7650685 | 49 | Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists. | J Med Chem 38: 3313-31 (1995) | Ciba-Geigy AG | 2D 3D TSV |
7650684 | 39 | Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. | J Med Chem 38: 3297-312 (1995) | Ciba-Geigy AG | 2D 3D TSV |
7650683 | 12 | Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol. | J Med Chem 38: 3287-96 (1995) | Royal Danish School of Pharmacy | 2D 3D TSV |
7650679 | 33 | Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines. | J Med Chem 38: 3258-63 (1995) | Sapienza University of Rome | 2D 3D TSV |
7650677 | 2 | A check on rational drug design: crystal structure of a complex of human immunodeficiency virus type 1 protease with a novel gamma-turn mimetic inhibitor. | J Med Chem 38: 3246-52 (1995) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7650675 | 25 | 9-substituted acridine derivatives with long half-life and potent antitumor activity: synthesis and structure-activity relationships. | J Med Chem 38: 3226-35 (1995) | Sloan-Kettering Institute for Cancer Research | 2D 3D TSV |
7650673 | 28 | (Aryloxy)methylsilane derivatives as new cholesterol biosynthesis inhibitors: synthesis and hypocholesterolemic activity of a new class of squalene epoxidase inhibitors. | J Med Chem 38: 3207-16 (1995) | Centre de Recherche Pierre Fabre | 2D 3D TSV |
7650672 | 24 | Keto/enol epoxy steroids as HIV-1 Tat inhibitors: structure-activity relationships and pharmacophore localization. | J Med Chem 38: 3197-206 (1995) | Sterling Winthrop Pharmaecuticals Research Division | 2D 3D TSV |
7650671 | 15 | Vinyl sulfones as mechanism-based cysteine protease inhibitors. | J Med Chem 38: 3193-6 (1995) | Khepri Pharmaceuticals, Inc. | 2D 3D TSV |
7650670 | 67 | 4-Aza-3-oxo-5 alpha-androst-1-ene-17 beta-N-aryl-carboxamides as dual inhibitors of human type 1 and type 2 steroid 5 alpha-reductases. Dramatic effect of N-aryl substituents on type 1 and type 2 5 alpha-reductase inhibitory potency. | J Med Chem 38: 3189-92 (1995) | Merck Research Laboratories | 2D 3D TSV |
7647964 | 71 | Characterization and distribution of putative 5-ht7 receptors in guinea-pig brain. | Br J Pharmacol 115: 107-16 (1995) | Syntex Discovery Research | 2D 3D TSV |
7636877 | 96 | Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells. | J Med Chem 38: 3146-55 (1995) | Ligand Pharmaceuticals Inc | 2D 3D TSV |
7636876 | 20 | (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses. | J Med Chem 38: 3138-45 (1995) | Pfizer Inc | 2D 3D TSV |
7636875 | 21 | Synthesis and dopaminergic activity of pyridine analogs of 5-hydroxy-2-(di-n-propylamino)tetralin. | J Med Chem 38: 3132-7 (1995) | Warner-Lambert Company | 2D 3D TSV |
7636873 | 62 | Aminoalkylindoles: structure-activity relationships of novel cannabinoid mimetics. | J Med Chem 38: 3094-105 (1995) | Sanofi Research Division | 2D 3D TSV |
7636872 | 24 | Chemistry and biology of the 2 beta-alkyl-3 beta-phenyl analogues of cocaine: subnanomolar affinity ligands that suggest a new pharmacophore model at the C-2 position. | J Med Chem 38: 3086-93 (1995) | Mayo Foundation | 2D 3D TSV |
7636870 | 18 | Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime. | J Med Chem 38: 3071-7 (1995) | University of Innsbruck | 2D 3D TSV |
7636869 | 11 | Synthesis and biological evaluation of a series of substituted benzo[a]phenanthridines as agonists at D1 and D2 dopamine receptors. | J Med Chem 38: 3062-70 (1995) | Purdue University | 2D 3D TSV |
7636868 | 51 | Diamine and triamine analogs and derivatives as inhibitors of deoxyhypusine synthase: synthesis and biological activity. | J Med Chem 38: 3053-61 (1995) | National Institute of Dental Research | 2D 3D TSV |
7636862 | 8 | Synthetic chemical diversity: solid phase synthesis of libraries of C2 symmetric inhibitors of HIV protease containing diamino diol and diamino alcohol cores. | J Med Chem 38: 2995-3002 (1995) | Abbott Laboratories | 2D 3D TSV |
7636861 | 32 | Synthesis and sigma binding properties of 1'- and 3'-halo- and 1',3'-dihalo-N-normetazocine analogues. | J Med Chem 38: 2986-9 (1995) | Research Triangle Institute | 2D 3D TSV |
7636860 | 48 | Synthesis and sigma binding properties of 2'-substituted 5,9 alpha-dimethyl-6,7-benzomorphans. | J Med Chem 38: 2978-85 (1995) | Research Triangle Institute | 2D 3D TSV |
7636858 | 25 | Flexible 1-[(2-aminoethoxy)alkyl]-3-ar(o)yl(thio)ureas as novel acetylcholinesterase inhibitors. Synthesis and biochemical evaluation. | J Med Chem 38: 2969-73 (1995) | Centre de Recherche Pierre Fabre | 2D 3D TSV |
7636854 | 22 | Balanced AT1/AT2 receptor antagonists. 4. XR510 and related 5-(3-amidopropanoyl)imidazoles possessing equal affinity for the AT1 and AT2 receptors. | J Med Chem 38: 2938-45 (1995) | DuPont Pharmaceuticals Company | 2D 3D TSV |
7636853 | 35 | 4-Diazinyl- and 4-pyridinylimidazoles: potent angiotensin II antagonists. A study of their activity and computational characterization. | J Med Chem 38: 2925-37 (1995) | Laboratori Guidotti S.p.A. | 2D 3D TSV |
7636851 | 19 | Farnesyl diphosphate-based inhibitors of Ras farnesyl protein transferase. | J Med Chem 38: 2906-21 (1995) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
7636849 | 52 | (E)-4-(2-[[3-(indol-5-yl)-1-oxo-2-butenyl]amino]phenoxy)butyric acid derivatives: a new class of steroid 5 alpha-reductase inhibitors in the rat prostate. 1. | J Med Chem 38: 2887-92 (1995) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
7636845 | 8 | Synthesis, structure elucidation, and biochemical evaluation of 7 alpha- and 7 beta-arylaliphatic-substituted androst-4-ene-3,17-diones as inhibitors of aromatase. | J Med Chem 38: 2842-50 (1995) | Ohio State University | 2D 3D TSV |
7636843 | 40 | Synthesis and structure-activity relationships of stilbene retinoid analogs substituted with heteroaromatic carboxylic acids. | J Med Chem 38: 2820-9 (1995) | Allergan Inc | 2D 3D TSV |
7636842 | 155 | Structure-activity relationships of the potent combined endothelin-A/endothelin-B receptor antagonist Ac-DDip16-Leu-Asp-Ile-Ile-Trp21: development of endothelin-B receptor selective antagonists. | J Med Chem 38: 2809-19 (1995) | Warner-Lambert Company | 2D 3D TSV |
7636841 | 16 | 5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety. | J Med Chem 38: 2802-8 (1995) | Pfizer Inc | 2D 3D TSV |
7636840 | 4 | Technetium-99m-labeled HOE 140: a potential bradykinin B2 receptor imaging agent. | J Med Chem 38: 2799-801 (1995) | Zentrale Pharmaforschung | 2D 3D TSV |
7629814 | 66 | Reversible inhibitors of the gastric (H+/K+)-ATPase. 5. Substituted 2,4-diaminoquinazolines and thienopyrimidines. | J Med Chem 38: 2763-73 (1995) | SmithKline Beecham Pharmaceuticals R&D | 2D 3D TSV |
7629813 | 125 | Reversible inhibitors of the gastric (H+/K+)-ATPase. 4. Identification of an inhibitor with an intermediate duration of action. | J Med Chem 38: 2748-62 (1995) | SmithKline Beecham Pharmaceuticals R&D | 2D 3D TSV |
7629811 | 19 | Novel angiotensin II receptor antagonists. Design, synthesis, and in vitro evaluation of dibenzo[a,d]cycloheptene and dibenzo[b,f]oxepin derivatives. Searching for bioisosteres of biphenylyltetrazole using a three-dimensional search technique. | J Med Chem 38: 2728-41 (1995) | Shionogi & Co., Ltd | 2D 3D TSV |
7629810 | 8 | Synthesis and biochemical evaluation of adenosylspermidine, a nucleoside-polyamine adduct inhibitor of spermidine synthase. | J Med Chem 38: 2714-27 (1995) | University of Michigan | 2D 3D TSV |
7629809 | 140 | Amino acid side chain descriptors for quantitative structure-activity relationship studies of peptide analogues. | J Med Chem 38: 2705-13 (1995) | University of Illinois at Chicago | 2D 3D TSV |
7629808 | 64 | Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies. | J Med Chem 38: 2692-704 (1995) | Universit£ di Siena | 2D 3D TSV |
7629802 | 48 | Structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase by 6-azaandrost-4-en-3-ones: optimization of the C17 substituent. | J Med Chem 38: 2621-7 (1995) | Glaxo Inc. Research Institute | 2D 3D TSV |
7629801 | 45 | 2,4-Diaminopyrido[3,2-d]pyrimidine inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii. | J Med Chem 38: 2615-20 (1995) | Institute | 2D 3D TSV |
7629799 | 32 | 1,1-Bisphosphonate squalene synthase inhibitors: interplay between the isoprenoid subunit and the diphosphate surrogate. | J Med Chem 38: 2596-605 (1995) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
7629797 | 73 | Inhibition of matrix metalloproteinases by hydroxamates containing heteroatom-based modifications of the P1' group. | J Med Chem 38: 2570-81 (1995) | Sterling Winthrop Pharmaceuticals Research Division | 2D 3D TSV |
7629795 | 13 | 4,5-Dihydro-3-(methanesulfonamidophenyl)-1-phenyl-1H-2,4-benzodiazepines: a novel class III antiarrhythmic agents. | J Med Chem 38: 2551-6 (1995) | Sterling Winthrop Research | 2D 3D TSV |
7629794 | 7 | Novel and potent adenosine 3',5'-cyclic phosphate phosphodiesterase III inhibitors: thiazolo[4,5-b][1,6]naphthyridin-2-ones. | J Med Chem 38: 2546-50 (1995) | Sterling Winthrop Pharmaceuticals Research Division | 2D 3D TSV |
7629791 | 5 | 5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3-f]indole: a novel 5-HT2C/5-HT2B receptor antagonist with improved affinity, selectivity, and oral activity. | J Med Chem 38: 2524-30 (1995) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7629790 | 32 | New orally active serine protease inhibitors. | J Med Chem 38: 2521-3 (1995) | Minase Research Institute | 2D 3D TSV |
7629789 | 8 | Synthesis, resolution, and biological evaluation of the four stereoisomers of 4-methylglutamic acid: selective probes of kainate receptors. | J Med Chem 38: 2518-20 (1995) | Symphony Pharmaceuticals, Inc. | 2D 3D TSV |
7623051 | 1 | A novel phorbol ester from Excoecaria agallocha. | J Nat Prod 58: 769-72 (1995) | National Cancer Institute | 2D 3D TSV |
7616416 | 11 | 7-(4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2(1H)-quinolinone (OPC-14597), a new putative antipsychotic drug with both presynaptic dopamine autoreceptor agonistic activity and postsynaptic D2 receptor antagonistic activity. | J Pharmacol Exp Ther 274: 329-36 (1995) | Third Tokushima Institute of New Drug Research | 2D 3D TSV |
7616392 | 5 | Functional characterization of the nonpeptide neurokinin3 (NK3) receptor antagonist, SR142801 on the human NK3 receptor expressed in Chinese hamster ovary cells. | J Pharmacol Exp Ther 274: 148-54 (1995) | Sanofi Recherche | 2D 3D TSV |
7608912 | 6 | (Piperidinylalkoxy)chromones: novel antihistamines with additional antagonistic activity against leukotriene D4. | J Med Chem 38: 2472-7 (1995) | Vrije Universiteit | 2D 3D TSV |
7608911 | 35 | Novel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase): potential agents for the treatment of prostatic cancer. | J Med Chem 38: 2463-71 (1995) | Institute of Cancer Research | 2D 3D TSV |
7608910 | 1 | Orally active beta-lactam inhibitors of human leukocyte elastase. 3. Stereospecific synthesis and structure-activity relationships for 3,3-dialkylazetidin-2-ones. | J Med Chem 38: 2449-62 (1995) | Merck Research Laboratories | 2D 3D TSV |
7608909 | 66 | [(Alkylamino)methyl]acrylophenones: potent and selective inhibitors of the epidermal growth factor receptor protein tyrosine kinase. | J Med Chem 38: 2441-8 (1995) | CIBA Limited | 2D 3D TSV |
7608907 | 6 | Synthesis and anti-HIV activity of 1,1'-dideoxygossypol and related compounds. | J Med Chem 38: 2427-32 (1995) | University of New Mexico School of Medicine | 2D 3D TSV |
7608905 | 24 | Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 1. Conformational constraint in the"message" sequence. | J Med Chem 38: 2410-7 (1995) | Oregon State University | 2D 3D TSV |
7608904 | 2 | Synthesis and evaluation of 6,7-dihydroxy-2,3,4,8,9,13b-hexahydro-1H- benzo[6,7]cyclohepta[1,2,3-ef][3]benzazepine, 6,7-dihydroxy- 1,2,3,4,8,12b-hexahydroanthr[10,4a,4-cd]azepine, and 10-(aminomethyl)-9,10- dihydro-1,2-dihydroxyanthracene as conformationally restricted analogs of beta-phenyldopamin | J Med Chem 38: 2395-409 (1995) | Purdue University | 2D 3D TSV |
7608903 | 29 | Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists. | J Med Chem 38: 2378-94 (1995) | Searle Research & Development | 2D 3D TSV |
7608902 | 53 | Sulfonylureas and sulfonylcarbamates as new non-tetrazole angiotensin II receptor antagonists. Discovery of a highly potent orally active (imidazolylbiphenylyl)sulfonylurea (HR 720). | J Med Chem 38: 2357-77 (1995) | Hoechst Roussel PGU Cardiovascular Agents | 2D 3D TSV |
7608901 | 78 | N-alkylated nitrogen-in-the-ring sugars: conformational basis of inhibition of glycosidases and HIV-1 replication. | J Med Chem 38: 2349-56 (1995) | Hokuriku University | 2D 3D TSV |
7608900 | 4 | Steroidal affinity labels of the estrogen receptor. 2. 17 alpha-[(Haloacetamido)alkyl]estradiols. | J Med Chem 38: 2339-48 (1995) | Centre de Recherche de l'INSERM | 2D 3D TSV |
7608899 | 5 | The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists. | J Med Chem 38: 2331-8 (1995) | Sandoz Pharma Limited | 2D 3D TSV |
7608898 | 4 | The serotonin 5-HT4 receptor. 1. Design of a new class of agonists and receptor map of the agonist recognition site. | J Med Chem 38: 2326-30 (1995) | Sandoz Pharma Limited | 2D 3D TSV |
7608895 | 61 | Conformationally defined 6-s-trans-retinoic acid analogs. 2. Selective agonists for nuclear receptor binding and transcriptional activity. | J Med Chem 38: 2302-10 (1995) | University of Alabama at Birmingham | 2D 3D TSV |
7608893 | 7 | Secondary interactions significantly removed from the sulfonamide binding pocket of carbonic anhydrase II influence inhibitor binding constants. | J Med Chem 38: 2286-91 (1995) | University of Pennsylvania | 2D 3D TSV |
7608891 | 7 | Potent inhibitors of proteasome. | J Med Chem 38: 2276-7 (1995) | Cephalon, Inc. | 2D 3D TSV |
7592911 | 37 | Cloning and functional expression of a human Y4 subtype receptor for pancreatic polypeptide, neuropeptide Y, and peptide YY. | J Biol Chem 270: 26762-5 (1995) | Synaptic Pharmaceutical Corporation | 2D 3D TSV |
7592910 | 36 | Expression cloning and pharmacological characterization of a human hippocampal neuropeptide Y/peptide YY Y2 receptor subtype. | J Biol Chem 270: 26758-61 (1995) | Synaptic Pharmaceutical Corporation | 2D 3D TSV |
7592745 | 12 | Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2. | J Biol Chem 270: 25672-7 (1995) | Medical College of Georgia | 2D 3D TSV |
7590751 | 11 | The cloning and chromosomal mapping of two novel human opioid-somatostatin-like receptor genes, GPR7 and GPR8, expressed in discrete areas of the brain. | Genomics 28: 84-91 (1995) | Addiction Research Foundation | 2D 3D TSV |
7582508 | 13 | The in vitro pharmacology of ZM 241385, a potent, non-xanthine A2a selective adenosine receptor antagonist. | Br J Pharmacol 115: 1096-102 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7582507 | 14 | RS 39604: a potent, selective and orally active 5-HT4 receptor antagonist. | Br J Pharmacol 115: 1087-95 (1995) | Syntex Discovery Research | 2D 3D TSV |
7582481 | 62 | The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors. | Br J Pharmacol 115: 622-8 (1995) | Syntex Discovery Research | 2D 3D TSV |
7568007 | 15 | Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel1b melatonin receptor. | Proc Natl Acad Sci U S A 92: 8734-8 (1995) | Massachusetts General Hospital | 2D 3D TSV |
7566488 | 30 | Different binding affinities of NMDA receptor channel blockers in various brain regions--indication of NMDA receptor heterogeneity. | Neuropharmacology 34: 533-40 (1995) | Merz Co. GmbH & Co. | 2D 3D TSV |
7562951 | 4 | Probing the hydrophobic pocket of the active site of aromatase with 4-phenoxy-7 alpha-(phenylthio)-4-androstene-3,17-dione. | J Med Chem 38: 4135-8 (1995) | University of Minnesota | 2D 3D TSV |
7562949 | 61 | Development of a potent thrombin receptor ligand. | J Med Chem 38: 4125-30 (1995) | Merck Research Laboratories | 2D 3D TSV |
7562946 | 7 | Synthesis and antiproliferative and antiviral activity of 2'-deoxy-2'-fluoroarabinofuranosyl analogs of the nucleoside antibiotics toyocamycin and sangivamycin. | J Med Chem 38: 4106-14 (1995) | University of Michigan | 2D 3D TSV |
7562944 | 16 | In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs. | J Med Chem 38: 4087-97 (1995) | University of Oklahoma | 2D 3D TSV |
7562941 | 20 | Design, synthesis, and structure-activity relationships of a new series of alpha-adrenergic agonists: spiro[(1,3-diazacyclopent-1-ene)-5,2'-(1',2',3',4'- tetrahydronaphthalene)]. | J Med Chem 38: 4056-69 (1995) | Institut de Recherches Servier | 2D 3D TSV |
7562940 | 34 | Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines. | J Med Chem 38: 4044-55 (1995) | Institut de Recherches Servier | 2D 3D TSV |
7562939 | 7 | Synthesis and anticonvulsant activity of enaminones. 3. Investigations on 4'-, 3'-, and 2'-substituted and polysubstituted anilino compounds, sodium channel binding studies, and toxicity evaluations. | J Med Chem 38: 4033-43 (1995) | Howard University | 2D 3D TSV |
7562938 | 17 | New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists. | J Med Chem 38: 4026-32 (1995) | Wyeth-Ayerst Research | 2D 3D TSV |
7562937 | 48 | Synthesis and biological evaluation of N6-cycloalkyl derivatives of 1-deazaadenine nucleosides: a new class of anti-human immunodeficiency virus agents. | J Med Chem 38: 4019-25 (1995) | Universit£ di Camerino | 2D 3D TSV |
7562936 | 10 | Synthesis of tight binding inhibitors and their action on the proprotein-processing enzyme furin. | J Med Chem 38: 4014-8 (1995) | Friedrich Miescher-Institut | 2D 3D TSV |
7562934 | 38 | Ribose-modified adenosine analogues as potential partial agonists for the adenosine receptor. | J Med Chem 38: 4000-6 (1995) | Leiden University | 2D 3D TSV |
7562933 | 24 | Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties. | J Med Chem 38: 3995-9 (1995) | Tohoku College of Pharmacy | 2D 3D TSV |
7562931 | 41 | Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles. | J Med Chem 38: 3972-82 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7562930 | 34 | Pseudodipeptide inhibitors of protein farnesyltransferase. | J Med Chem 38: 3967-71 (1995) | Merck Research Laboratories | 2D 3D TSV |
7562928 | 35 | Chiral dioxolane inhibitors of leukotriene biosynthesis: structure-activity relationships and syntheses using asymmetric dihydroxylation. | J Med Chem 38: 3951-6 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7562926 | 81 | Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors. | J Med Chem 38: 3933-40 (1995) | National Institutes of Health | 2D 3D TSV |
7562924 | 10 | Resolution and in vitro and initial in vivo evaluation of isomers of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate: a high-affinity ligand for the muscarinic receptor. | J Med Chem 38: 3908-17 (1995) | Oak Ridge National Laboratory (ORNL) | 2D 3D TSV |
7562922 | 48 | Antiinflammatory 4,5-diarylpyrroles. 2. Activity as a function of cyclooxygenase-2 inhibition. | J Med Chem 38: 3895-901 (1995) | DuPont Pharmaceuticals Company | 2D 3D TSV |
7562919 | 132 | Inhibition of monoamine oxidase-B by 5H-indeno[1,2-c]pyridazines: biological activities, quantitative structure-activity relationships (QSARs) and 3D-QSARs. | J Med Chem 38: 3874-83 (1995) | Université de Lausanne | 2D 3D TSV |
7562916 | 49 | Inhibition of uridine phosphorylase: synthesis and structure-activity relationships of aryl-substituted 5-benzyluracils and 1-[(2-hydroxyethoxy)methyl]-5-benzyluracils. | J Med Chem 38: 3850-6 (1995) | Burroughs Wellcome Co. | 2D 3D TSV |
7562915 | 78 | Synthesis and structure-activity relationships of analogs of 2'-deoxy-2'-(3-methoxybenzamido)adenosine, a selective inhibitor of trypanosomal glycosomal glyceraldehyde-3-phosphate dehydrogenase. | J Med Chem 38: 3838-49 (1995) | University of Ghent | 2D 3D TSV |
7562910 | 18 | Effect of bridge region variation on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines. | J Med Chem 38: 3798-805 (1995) | Duquesne University | 2D 3D TSV |
7562908 | 46 | Tyrosine kinase inhibitors. 7. 7-Amino-4-(phenylamino)- and 7-amino-4-[(phenylmethyl)amino]pyrido[4,3-d]pyrimidines: a new class of inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor. | J Med Chem 38: 3780-8 (1995) | University of Auckland | 2D 3D TSV |
7562907 | 33 | New spiropiperidines as potent and selective non-peptide tachykinin NK2 receptor antagonists. | J Med Chem 38: 3772-9 (1995) | Glaxo Wellcome Medicines Research Centre | 2D 3D TSV |
7562906 | 3 | Derivatives of 5-[[1-(4'-carboxybenzyl)imidazolyl]methylidene]hydantoins as orally active angiotensin II receptor antagonists. | J Med Chem 38: 3759-71 (1995) | Warner-Lambert Company | 2D 3D TSV |
7562905 | 258 | Potent and orally active angiotensin II receptor antagonists with equal affinity for human AT1 and AT2 subtypes. | J Med Chem 38: 3741-58 (1995) | Merck Research Laboratories | 2D 3D TSV |
7562904 | 64 | Synthesis of 1,4,7,8,9,10-hexahydro-9-methyl-6-nitropyrido[3,4-f]- quinoxaline-2,3-dione and related quinoxalinediones: characterization of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (and N-methyl-D-aspartate) receptor and anticonvulsant activity. | J Med Chem 38: 3720-40 (1995) | Warner-Lambert Company | 2D 3D TSV |
7562903 | 10 | 1-Aminoindan-1,5-dicarboxylic acid: a novel antagonist at phospholipase C-linked metabotropic glutamate receptors. | J Med Chem 38: 3717-9 (1995) | Università di Perugia | 2D 3D TSV |
7562902 | 114 | Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. | J Med Chem 38: 3681-716 (1995) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7562598 | 1 | Cepharanthin, a multidrug resistant modifier, is a substrate for P-glycoprotein. | J Pharmacol Exp Ther 275: 73-8 (1995) | Kyoto University Hospital | 2D 3D TSV |
7562497 | 127 | Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception. | J Pharmacol Exp Ther 274: 1263-70 (1995) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
7562491 | 10 | Pharmacological characterization of a new class of nonpeptide neurokinin A antagonists that demonstrate species selectivity. | J Pharmacol Exp Ther 274: 1216-21 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7562467 | 11 | Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, U-97018. | J Pharmacol Exp Ther 274: 1042-53 (1995) | Upjohn Pharmaceuticals Limited | 2D 3D TSV |
7561907 | 1 | Barceloneic acid A, a new farnesyl-protein transferase inhibitor from a Phoma species. | J Nat Prod 58: 986-91 (1995) | Merck Research Laboratories | 2D 3D TSV |
7561897 | 17 | A reinvestigation of Maprounea triterpenes. | J Nat Prod 58: 1039-46 (1995) | National Cancer Institute | 2D 3D TSV |
7561895 | 4 | Mechanistic Evaluation of New Plant-Derived Compounds That Inhibit HIV-1 Reverse Transcriptase | J Nat Prod 58: 1024-1031 (1995) | TBA | 2D 3D TSV |
7559383 | 11 | Cloning and functional expression of a cDNA encoding a human type 2 neuropeptide Y receptor. | J Biol Chem 270: 22661-4 (1995) | Bristol-Myers Squibb Co. | 2D 3D TSV |
7543579 | 46 | Novel, potent, and orally active substance P antagonists: synthesis and antagonist activity of N-benzylcarboxamide derivatives of pyrido[3,4-b]pyridine. | J Med Chem 38: 3106-20 (1995) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
7543578 | 6 | Anti-AIDS (acquired immune deficiency syndrome) agents. 17. New brominated hexahydroxybiphenyl derivatives as potent anti-HIV agents. | J Med Chem 38: 3003-8 (1995) | University of North Carolina at Chapel Hill | 2D 3D TSV |
7540209 | 11 | Design and synthesis of novel inhibitors of HIV-1 reverse transcriptase. | J Med Chem 38: 2145-51 (1995) | State University of New York | 2D 3D TSV |
7540208 | 10 | Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. | J Med Chem 38: 2038-40 (1995) | Tosoh Company, Ltd. | 2D 3D TSV |
7540207 | 56 | Novel inhibitors of potassium ion channels on human T lymphocytes. | J Med Chem 38: 1877-83 (1995) | Sanofi Winthrop Inc. | 2D 3D TSV |
7538590 | 28 | Benzophenone derivatives: a novel series of potent and selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase. | J Med Chem 38: 1657-65 (1995) | Glaxo Research and Development Limited | 2D 3D TSV |
7537334 | 18 | Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 3. Dipyrido[2,3-b:2',3'-e]diazepinones. | J Med Chem 38: 1406-10 (1995) | Boehringer Ingelheim Pharmaceuticals Inc | 2D 3D TSV |
7535424 | 29 | Characterization of somatostatin receptor subtypes controlling rat gastric acid and pancreatic amylase release. | Peptides 15: 1421-4 (1994) | Tulane University | 2D 3D TSV |
7535362 | 39 | Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan. | J Med Chem 38: 934-41 (1995) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
7530773 | 31 | Derivatives of cis-2-amino-8-hydroxy-1-methyltetralin: mixed 5-HT1A-receptor agonists and dopamine D2-receptor antagonists. | J Med Chem 38: 150-60 (1995) | Uppsala University | 2D 3D TSV |
7528281 | 30 | Inhibition of peptidylglycine alpha-amidating monooxygenase by N-substituted homocysteine analogs. | J Med Chem 37: 4430-7 (1995) | Ciba-Geigy Corporation | 2D 3D TSV |
7528269 | 2 | 1'-(2-Phenyl-ethylene)-ditryptophenaline, a New Dimeric Diketopiperazine from Aspergillus flavus | J Nat Prod 57: 1239-1244 (1994) | TBA | 2D 3D TSV |
7527861 | 3 | Importance of parallel vectors and"hydrophobic collapse" of the aligned aromatic rings: discovery of a potent substance P antagonist. | J Med Chem 37: 4263-6 (1995) | Pfizer Inc | 2D 3D TSV |
7525961 | 12 | L-N6-(1-iminoethyl)lysine: a selective inhibitor of inducible nitric oxide synthase. | J Med Chem 37: 3886-8 (1994) | G. D. Searle Research and Development | 2D 3D TSV |
7525960 | 2 | The synthesis of nucleoside 5'-O-(1,1-dithiotriphosphates). | J Med Chem 37: 3850-4 (1994) | Polish Academy of Sciences | 2D 3D TSV |
7525878 | 3 | New lignans from Anogeissus acuminata with HIV-1 reverse transcriptase inhibitory activity. | J Nat Prod 57: 896-904 (1994) | College of Pharmacy | 2D 3D TSV |
7523675 | 3 | Synthesis and evaluation of the anti-HIV activity of aza and deaza analogues of isoddA and their phosphates as prodrugs. | J Med Chem 37: 3534-41 (1994) | Universit£ di Camerino | 2D 3D TSV |
7523674 | 1 | Structure--activity relationships of sialyl Lewis x-containing oligosaccharides. 1. Effect of modifications of the fucose moiety. | J Med Chem 37: 3459-63 (1994) | Cytel Corporation | 2D 3D TSV |
7523657 | 14 | Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity. | J Pharmacol Exp Ther 270: 1270-81 (1994) | Eli Lilly and Company | 2D 3D TSV |
7520943 | 16 | Aza-tricyclic substance P antagonists. | J Med Chem 37: 2831-40 (1994) | Pfizer Inc | 2D 3D TSV |
7520908 | 64 | Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. | J Clin Psychiatry 5-12 (1994) | Janssen Research Foundation | 2D 3D TSV |
7520080 | 18 | Synthesis of naphthalenesulfonic acid small molecules as selective inhibitors of the DNA polymerase and ribonuclease H activities of HIV-1 reverse transcriptase. | J Med Chem 37: 2513-9 (1994) | College of Pharmacy | 2D 3D TSV |
7520079 | 13 | Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. | J Med Chem 37: 2437-44 (1994) | Merck Research Laboratories | 2D 3D TSV |
7518523 | 90 | Identification of tricyclic analogs related to ellagic acid as potent/selective tyrosine protein kinase inhibitors. | J Med Chem 37: 2224-31 (1994) | Pfizer Inc | 2D 3D TSV |
7518522 | 12 | Comparison of the conformation of active and nonactive backbone cyclic analogs of substance P as a tool to elucidate features of the bioactive conformation: NMR and molecular dynamics in DMSO and water. | J Med Chem 37: 2145-52 (1994) | Technische Universität München | 2D 3D TSV |
7518514 | 46 | (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization. | J Pharmacol Exp Ther 270: 310-8 (1994) | Abbott Laboratories | 2D 3D TSV |
7518496 | 9 | Cloning and expression of a 5-hydroxytryptamine7 receptor positively coupled to adenylyl cyclase. | J Neurochem 63: 456-64 (1994) | Syntex Discovery Research | 2D 3D TSV |
7518002 | 38 | Studies on neurokinin antagonists. 4. Synthesis and structure-activity relationships of novel dipeptide substance P antagonists: N2-[(4R)-4-hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl]-N- methyl-N-(phenylmethyl)-3-(2-naphthyl)-L-alaninamide and its related compounds. | J Med Chem 37: 2090-9 (1994) | Fujisawa Pharmaceutical Co., Ltd | 2D 3D TSV |
7518001 | 5 | Approaches toward selective inhibition of nitric oxide synthase. | J Med Chem 37: 1899-907 (1994) | University of Michigan | 2D 3D TSV |
7517439 | 2 | Spiroquinazoline, a Novel Substance P Inhibitor with a New Carbon Skeleton, Isolated from Aspergillus flavipes | J Nat Prod 57: 471-476 (1994) | TBA | 2D 3D TSV |
7515823 | 54 | Actions of phenylglycine analogs at subtypes of the metabotropic glutamate receptor family. | Eur J Pharmacol 267: 77-84 (1994) | Novo Nordisk A/S | 2D 3D TSV |
7515443 | 79 | Design and synthesis of side-chain conformationally restricted phenylalanines and their use for structure-activity studies on tachykinin NK-1 receptor. | J Med Chem 37: 1586-601 (1994) | Universit£ P. et M. Curie | 2D 3D TSV |
7515442 | 9 | 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. | J Med Chem 37: 1578-85 (1994) | Institute | 2D 3D TSV |
7515410 | 8 | Pentacyclic triterpenes derived from Maprounea africana are potent inhibitors of HIV-1 reverse transcriptase. | J Nat Prod 57: 415-8 (1994) | University of Illinois at Chicago | 2D 3D TSV |
7514263 | 1 | Direct demonstration of high affinity interactions of immunosuppressant drugs with the drug binding site of the human P-glycoprotein. | Mol Pharmacol 45: 773-6 (1994) | University of North Carolina | 2D 3D TSV |
7513763 | 92 | Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor. | J Med Chem 37: 1269-74 (1994) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
7512140 | 5 | Resolution, absolute stereochemistry, and pharmacology of the S-(+)- and R-(-)-isomers of the apparent partial AMPA receptor agonist (R,S)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid [(R,S)-APPA]. | J Med Chem 37: 878-84 (1994) | Royal Danish School of Pharmacy | 2D 3D TSV |
7510786 | 24 | Hexaprenoid hydroquinones, novel inhibitors of the reverse transcriptase of human immunodeficiency virus type 1. | J Nat Prod 56: 2120-5 (1993) | Sackler School of Medicine | 2D 3D TSV |
7510341 | 51 | In vitro and in vivo activities of reduced-size antagonists of luteinizing hormone-releasing hormone. | J Med Chem 37: 701-5 (1994) | TAP Pharmaceuticals, Inc. | 2D 3D TSV |
7510340 | 47 | Tyrosine kinase inhibitors. 2. Synthesis of 2,2'-dithiobis(1H-indole-3-alkanamides) and investigation of their inhibitory activity against epidermal growth factor receptor and pp60v-src protein tyrosine kinases. | J Med Chem 37: 598-609 (1994) | University of Auckland | 2D 3D TSV |
7509389 | 8 | Pharmacological profile of FK480, a novel cholecystokinin type-A receptor antagonist: comparison to loxiglumide. | J Pharmacol Exp Ther 268: 571-5 (1994) | Fujisawa Pharmaceutical Co., Ltd | 2D 3D TSV |
7508512 | 21 | Structure determination, pharmacological evaluation, and structure-activity studies of a new cyclic peptide substance P antagonist containing the new amino acid 3-prenyl-beta-hydroxytyrosine, isolated from Aspergillus flavipes. | J Med Chem 37: 356-63 (1994) | Sterling Winthrop Pharmaceuticals Research Division | 2D 3D TSV |
7507528 | 23 | Enhanced selectivity of oxytocin antagonists containing sarcosine in position 7. | J Med Chem 37: 255-9 (1994) | Max-Planck-Institut f£r Biophysik | 2D 3D TSV |
7507165 | 139 | Design and synthesis of novel cyclic RGD-containing peptides as highly potent and selective integrin alpha IIb beta 3 antagonists. | J Med Chem 37: 1-8 (1994) | Telios Pharmaceuticals, Inc. | 2D 3D TSV |
7506312 | 36 | Derivatives of 2-(dipropylamino)tetralin: effect of the C8-substituent on the interaction with 5-HT1A receptors. | J Med Chem 36: 4221-9 (1994) | Uppsala University | 2D 3D TSV |
7506311 | 18 | The inophyllums, novel inhibitors of HIV-1 reverse transcriptase isolated from the Malaysian tree, Calophyllum inophyllum Linn. | J Med Chem 36: 4131-8 (1994) | SmithKline Beecham Pharmaceuticals R&D | 2D 3D TSV |
7504733 | 33 | Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines. | J Med Chem 36: 3784-94 (1993) | Glaxo Group Research Ltd. | 2D 3D TSV |
7495840 | 10 | Proton/peptide cotransporter (PEPT 2) from human kidney: functional characterization and chromosomal localization. | Biochim Biophys Acta 1240: 1-4 (1996) | Medical College of Georgia | 2D 3D TSV |
7494145 | 5 | Enzyme Inhibitors: New and Known Polybrominated Phenols and Diphenyl Ethers from Four Indo-Pacific Dysidea Sponges | J Nat Prod 58: 1384-1391 (1995) | TBA | 2D 3D TSV |
7490734 | 9 | Design and synthesis of conformationally constrained analogues of 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as potent inhibitors of cAMP-specific phosphodiesterase. | J Med Chem 38: 4848-54 (1996) | Glaxo Wellcome Research | 2D 3D TSV |
7490733 | 59 | Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 5. 4-Substituted and 2,4-disubstituted analogs of nevirapine. | J Med Chem 38: 4839-47 (1995) | Boehringer Ingelheim Pharmaceuticals Inc | 2D 3D TSV |
7490732 | 120 | Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes. | J Med Chem 38: 4830-8 (1995) | Boehringer Ingelheim Pharmaceuticals Inc | 2D 3D TSV |
7490731 | 45 | Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds. | J Med Chem 38: 4821-9 (1996) | Eisai Company, Ltd | 2D 3D TSV |
7490730 | 20 | N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists. | J Med Chem 38: 4806-20 (1996) | Istituto Lusofarmaco | 2D 3D TSV |
7490729 | 62 | Identification of a series of 3-(benzyloxy)-1-azabicyclo[2.2.2]octane human NK1 antagonists. | J Med Chem 38: 4793-805 (1996) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
7490728 | 87 | Selective and potent monoamine oxidase type B inhibitors: 2-substituted 5-aryltetrazole derivatives. | J Med Chem 38: 4786-92 (1996) | Université Paris 7 | 2D 3D TSV |
7490727 | 72 | (E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype. | J Med Chem 38: 4776-85 (1996) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
7490726 | 10 | (R)-(+)-N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl- 2-propynyl]-N-hydroxyurea (ABT-761), a second-generation 5-lipoxygenase inhibitor. | J Med Chem 38: 4768-75 (1996) | Abbott Laboratories | 2D 3D TSV |
7490725 | 9 | Synthesis and characterization of a highly potent and effective antagonist of retinoic acid receptors. | J Med Chem 38: 4764-7 (1996) | Allergan Inc | 2D 3D TSV |
7490724 | 11 | N-[(1-butyl-4-piperidinyl)methyl]-3,4dihydro-2H-[1,3]oxazino[3,2- a]indole10-carboxamide hydrochloride: the first potent and selective 5-HT4 receptor antagonist amide with oral activity. | J Med Chem 38: 4760-3 (1996) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
7490723 | 37 | New drug developments for opportunistic infections in immunosuppressed patients: Pneumocystis carinii. | J Med Chem 38: 4739-59 (1996) | Indiana University School of Medicine | 2D 3D TSV |
7473601 | 11 | A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affinity of 6-arylpyrrolo[2,1-d][1,5]benzothiazepines toward mitochondrial benzodiazepine receptors. | J Med Chem 38: 4730-8 (1995) | Universit£ di Ferrara | 2D 3D TSV |
7473600 | 11 | Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities. | J Med Chem 38: 4720-9 (1995) | University of Arizona | 2D 3D TSV |
7473599 | 10 | Synthesis and antimicrobial and toxicological studies of amino acid and peptide derivatives of kanamycin A and netilmicin. | J Med Chem 38: 4710-9 (1995) | Agricultural University of Athens | 2D 3D TSV |
7473597 | 33 | Inhibition of the EGF-stimulated cellular proliferation of ER 22 cells by hydroxybiphenyl derivatives. | J Med Chem 38: 4693-703 (1995) | University of Paris | 2D 3D TSV |
7473596 | 35 | A novel class of cyclic beta-dicarbonyl leaving groups and their use in the design of benzisothiazolone human leukocyte elastase inhibitors. | J Med Chem 38: 4687-92 (1995) | Sterling Winthrop Pharmaceuticals Research Division | 2D 3D TSV |
7473595 | 12 | A new series of pyridinone derivatives as potent non-nucleoside human immunodeficiency virus type 1 specific reverse transcriptase inhibitors. | J Med Chem 38: 4679-86 (1995) | Institut Curie | 2D 3D TSV |
7473594 | 11 | 4-(Heteroarylthio)-2-biphenylyltetrazoles as nonpeptide angiotensin II antagonists. | J Med Chem 38: 4670-8 (1995) | Burroughs Wellcome Co. | 2D 3D TSV |
7473592 | 2 | Design, synthesis, and structure-activity relationship of novel dinucleotide analogs as agents against herpes and human immunodeficiency viruses. | J Med Chem 38: 4648-59 (1995) | Academia Sinica | 2D 3D TSV |
7473590 | 37 | 1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist. | J Med Chem 38: 4634-6 (1995) | Merck Research Laboratories | 2D 3D TSV |
7473585 | 70 | 1,2-Diarylcyclopentenes as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents. | J Med Chem 38: 4570-8 (1995) | Searle Research and Development | 2D 3D TSV |
7473584 | 16 | alpha-Hydroxy phosphinyl-based inhibitors of human renin. | J Med Chem 38: 4557-69 (1995) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
7473582 | 29 | Thiopyranol[2,3,4-c,d]indoles as inhibitors of 5-lipoxygenase, 5-lipoxygenase-activating protein, and leukotriene C4 synthase. | J Med Chem 38: 4538-47 (1995) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
7473577 | 11 | 5-Arylthio-substituted 2-amino-4-oxo-6-methylpyrrolo[2,3-d]pyrimidine antifolates as thymidylate synthase inhibitors and antitumor agents. | J Med Chem 38: 4495-502 (1995) | Duquesne University | 2D 3D TSV |
7473573 | 47 | Structure-based design of nonpeptidic HIV protease inhibitors from a cyclooctylpyranone lead structure. | J Med Chem 38: 4463-73 (1995) | Upjohn Laboratories | 2D 3D TSV |
7473572 | 28 | Quantitative structure-activity relationships (QSARs) of N-terminus fragments of NK1 tachykinin antagonists: a comparison of classical QSARs and three-dimensional QSARs from similarity matrices. | J Med Chem 38: 4454-62 (1995) | Cambridge University Forvie Site | 2D 3D TSV |
7473571 | 90 | Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions. | J Med Chem 38: 4446-53 (1995) | Eli Lilly and Company | 2D 3D TSV |
7473570 | 4 | Kynurenic acid derivatives inhibit the binding of nerve growth factor (NGF) to the low-affinity p75 NGF receptor. | J Med Chem 38: 4439-45 (1995) | Warner-Lambert Company | 2D 3D TSV |
7473568 | 5 | Synthetic and structure/activity studies on acid-substituted 2-arylphenols: discovery of 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5- hydroxyphenoxy]-propoxy]phenoxy]benzoic acid, a high-affinity leukotriene B4 receptor antagonist. | J Med Chem 38: 4411-32 (1995) | Eli Lilly and Company | 2D 3D TSV |
7473567 | 7 | Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity. | J Med Chem 38: 4393-410 (1995) | Università di Siena | 2D 3D TSV |
7473566 | 152 | Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. | J Med Chem 38: 4380-92 (1995) | H. Lundbeck A/S | 2D 3D TSV |
7473562 | 11 | Synthesis of isoornithines and methylputrescines. An evaluation of their inhibitory effects on ornithine decarboxylase. | J Med Chem 38: 4337-41 (1995) | Universidad de Buenos Aires | 2D 3D TSV |
7473559 | 85 | Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists. | J Med Chem 38: 4309-24 (1995) | Tsukuba Research Institute | 2D 3D TSV |
7473558 | 12 | A series of N4-imidoethyl derivatives of 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine as 5-HT1A receptor ligands: synthesis and structure-affinity relationships. | J Med Chem 38: 4303-8 (1995) | Solvay Duphar Research Laboratories | 2D 3D TSV |
7473557 | 65 | Improving the affinity and selectivity of a nonpeptide series of cholecystokinin-B/gastrin receptor antagonists based on the dibenzobicyclo[2.2.2]octane skeleton. | J Med Chem 38: 4294-302 (1995) | James Black Foundation | 2D 3D TSV |
7473556 | 30 | (+/-)-(N-alkylamino)benzazepine analogs: novel dopamine D1 receptor antagonists. | J Med Chem 38: 4284-93 (1995) | National Institutes of Health | 2D 3D TSV |
7473554 | 7 | L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides. | J Med Chem 38: 4270-5 (1995) | National Cancer Institute-Bethesda | 2D 3D TSV |
7473548 | 74 | N-aryl-N'-benzylpiperazines as potential antipsychotic agents. | J Med Chem 38: 4211-22 (1995) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
7473547 | 103 | Piperazinylalkyl heterocycles as potential antipsychotic agents. | J Med Chem 38: 4198-210 (1995) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
7473546 | 61 | Esters of 3-pyridylacetic acid that combine potent inhibition of 17 alpha-hydroxylase/C17,20-lyase (cytochrome P45017 alpha) with resistance to esterase hydrolysis. | J Med Chem 38: 4191-7 (1995) | CRC Laboratory | 2D 3D TSV |
7473544 | 32 | Hydroxylated aromatic inhibitors of HIV-1 integrase. | J Med Chem 38: 4171-8 (1995) | National Cancer Institute-Bethesda | 2D 3D TSV |
7473543 | 5 | Cyclosporin analogs modified in the 3,7,8-positions: substituent effects on peptidylprolyl isomerase inhibition and immunosuppressive activity are nonadditive. | J Med Chem 38: 4164-70 (1995) | University of Wisconsin-Madison | 2D 3D TSV |
7473541 | 26 | Phenoxypropylamines: a new series of squalene synthase inhibitors. | J Med Chem 38: 4157-60 (1995) | Zeneca Pharmaceuticals | 2D 3D TSV |
7473144 | 1 | Pharmacological characterization of GT-2016, a non-thiourea-containing histamine H3 receptor antagonist: in vitro and in vivo studies. | J Pharmacol Exp Ther 275: 598-604 (1995) | Gliatech Inc | 2D 3D TSV |
7452682 | 76 | 3-(4-Piperidinylalkyl)indoles, selective inhibitors of neuronal 5-hydroxytryptamine uptake. | J Med Chem 23: 1306-10 (1981) | TBA | 2D 3D TSV |
7452681 | 81 | Thrombin inhibitors. 3. Carboxyl-containing amide derivatives of N alpha-substituted L-arginine. | J Med Chem 23: 1293-9 (1981) | TBA | 2D 3D TSV |
7420361 | 1 | (+/-)-trans-2-(Aminomethyl)cyclobutanecarboxylic acid hydrochloride: a rigid analogue of gamma-aminobutyric acid. | J Med Chem 23: 1142-4 (1980) | TBA | 2D 3D TSV |
7411554 | 20 | Demethyl analogues of psychoactive methoxyphenalkylamines: synthesis and serotonin receptor affinities. | J Med Chem 23: 990-4 (1980) | TBA | 2D 3D TSV |
7401110 | 109 | Thrombin inhibitors. 2. Amide derivatives of N alpha-substituted L-arginine. | J Med Chem 23: 830-6 (1980) | TBA | 2D 3D TSV |
7401109 | 32 | Thrombin inhibitors. 1. Ester derivatives of N alpha-(arylsulfonyl)-L-arginine. | J Med Chem 23: 827-30 (1980) | TBA | 2D 3D TSV |
7401106 | 21 | Heat-induced formation of alpha,beta-unsaturated nucleoside dialdehydes and their activity with adenosine deaminase. | J Med Chem 23: 795-8 (1980) | TBA | 2D 3D TSV |
7401098 | 11 | Synthesis of 1,3-diazepin-2-one nucleosides as transition-state inhibitors of cytidine deaminase. | J Med Chem 23: 713-5 (1980) | TBA | 2D 3D TSV |
7381854 | 9 | Structure--antitubulin activity relationship in steganacin congeners and analogues. Inhibition of tubulin polymerization in vitro by (+/-)-isodeoxypodophyllotoxin. | J Med Chem 23: 546-9 (1980) | TBA | 2D 3D TSV |
7381849 | 18 | Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 1. Chloro-substituted 1,2,3,4-tetrahydroisoquinolines. | J Med Chem 23: 506-11 (1980) | TBA | 2D 3D TSV |
7365749 | 2 | Convenient synthesis of 10-deazaaminopterin via a pteridine ylide. | J Med Chem 23: 320-1 (1980) | TBA | 2D 3D TSV |
7365745 | 8 | Cyclophosphamide potentiation and aldehyde oxidase inhibition by phosphorylated aldehydes and acetals. | J Med Chem 23: 300-4 (1980) | TBA | 2D 3D TSV |
7359525 | 3 | Inhibitors of polyamine biosynthesis. 8. Irreversible inhibition of mammalian S-adenosyl-L-methionine decarboxylase by substrate analogues. | J Med Chem 23: 121-7 (1980) | TBA | 2D 3D TSV |
7332706 | 24 | 2,3-Dihydrobenzofuran-2-ones: a new class of highly potent antiinflammatory agents. | J Med Chem 24: 1465-71 (1981) | TBA | 2D 3D TSV |
7328589 | 8 | (alpha S)-erythro-alpha-methylepinephrine: preparation and stereoselective binding to adrenergic receptors in rat forebrain. | J Med Chem 24: 1261-3 (1981) | TBA | 2D 3D TSV |
7328588 | 9 | Synthesis and adrenoceptor affinity of some highly polar beta-substituted catecholamines. | J Med Chem 24: 1258-60 (1981) | TBA | 2D 3D TSV |
7328576 | 6 | Interaction of 1-(5-phospho-beta-D-arabinofuranosyl)-5-substituted-uracils with thymidylate synthetase: mechanism-based inhibition by 1-(5-phospho-beta-D-arabinosyl)-5-fluorouracil. | J Med Chem 24: 1161-5 (1982) | TBA | 2D 3D TSV |
7310833 | 14 | Interaction of aromatic dyes with the coenzyme A binding site of choline acetyltransferase. | J Med Chem 24: 1534-7 (1982) | TBA | 2D 3D TSV |
7310821 | 31 | Aporphines, 36. Dopamine receptor interactions of trihydroxyaporphines. Synthesis, radioreceptor binding, and striatal adenylate cyclase stimulation of 2,10,11-trihydroxyaporphines in comparison with other hydroxylated aporphines. | J Med Chem 24: 1440-5 (1981) | TBA | 2D 3D TSV |
7310818 | 20 | Photoelectron spectra of psychotropic drugs. 6. Relationships between the physical properties and pharmacological actions of amphetamine analogues. | J Med Chem 24: 1414-21 (1982) | TBA | 2D 3D TSV |
7310814 | 7 | Adenosine deaminase inhibitors. Conversion of a single chiral synthon into erythro- and threo-9-(2-hydroxy-3-nonyl)adenines. | J Med Chem 24: 1383-5 (1982) | TBA | 2D 3D TSV |
7310803 | 4 | Synthesis and evaluation of some stable multisubstrate adducts as specific inhibitors of spermidine synthase. | J Med Chem 24: 1277-84 (1982) | TBA | 2D 3D TSV |
7310802 | 6 | Synthesis and evaluation of some stable multisubstrate adducts as inhibitors of catechol O-methyltransferase. | J Med Chem 24: 1271-7 (1982) | TBA | 2D 3D TSV |
7288824 | 1 | Synthesis of 5,11-methenyltetrahydrohomofolate and its antifolate activity in vitro. | J Med Chem 24: 1086-8 (1981) | TBA | 2D 3D TSV |
7288815 | 18 | Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. | J Med Chem 24: 1021-6 (1981) | TBA | 2D 3D TSV |
7277385 | 39 | Inhibition of dihydrofolate reductase: structure-activity correlations of quinazolines based upon molecular shape analysis. | J Med Chem 24: 812-8 (1981) | TBA | 2D 3D TSV |
7252985 | 16 | Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 3. Bis[tetrahydroisoquinoline]s. | J Med Chem 24: 756-9 (1981) | TBA | 2D 3D TSV |
7252974 | 11 | Cyclic urea nucleosides. Cytidine deaminase activity as a function of aglycon ring size. | J Med Chem 24: 662-6 (1981) | TBA | 2D 3D TSV |
7241506 | 40 | New analgesic drugs derived from phencyclidine. | J Med Chem 24: 496-9 (1981) | TBA | 2D 3D TSV |
7205880 | 69 | Importance of the aromatic ring in adrenergic amines. 5. Nonaromatic analogues of phenylethanolamine as inhibitors of phenylethanolamine N-methyltransferase: role of hydrophobic and steric interactions. | J Med Chem 24: 7-12 (1981) | TBA | 2D 3D TSV |
7205869 | 9 | Importance of the aromatic ring in adrenergic amines. 6. Nonaromatic analogues of phenylethanolamine as inhibitors of phenylethanolamine N-methyltransferase: role of pi-electronic and steric interactions. | J Med Chem 24: 12-6 (1981) | TBA | 2D 3D TSV |
7200145 | 22 | Synthesis and dopaminergic properties of some exo- and endo-2-aminobenzonorbornenes designed as rigid analogue of dopamine. | J Med Chem 25: 363-8 (1982) | TBA | 2D 3D TSV |
7200144 | 2 | (+/-)-4-Aryl-4,5-dihydro-3H-1,3-benzodiazepines. 1. Synthesis and evaluation of (+/-)-4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine and analogues as potential antidepressant agents. | J Med Chem 25: 340-6 (1982) | TBA | 2D 3D TSV |
7199089 | 25 | Highly selective inhibitors of thromboxane synthetase. 2. Pyridine derivatives. | J Med Chem 24: 1149-55 (1982) | TBA | 2D 3D TSV |
7199088 | 50 | Highly selective inhibitors of thromboxane synthetase. 1. Imidazole derivatives. | J Med Chem 24: 1139-48 (1982) | TBA | 2D 3D TSV |
7154006 | 34 | 2-Amino-6-chloro-4-(N-methylpiperazino)pyrimidines, inhibitors of spiroperidol binding. | J Med Chem 25: 1459-65 (1982) | TBA | 2D 3D TSV |
7154005 | 27 | Conformationally restricted congeners of dopamine derived from 2-aminoindan. | J Med Chem 25: 1442-6 (1982) | TBA | 2D 3D TSV |
7154003 | 7 | A quantitative structure-activity relationship study of the inhibitory action of a series of enkephalin-like peptides in the guinea pig ileum and mouse vas deferens bioassays. | J Med Chem 25: 1428-31 (1983) | TBA | 2D 3D TSV |
7154002 | 8 | Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates and opioid peptides. | J Med Chem 25: 1423-7 (1983) | TBA | 2D 3D TSV |
7143367 | 3 | Importance of the aromatic ring in adrenergic amines. 8. 2-(Aminomethyl)-trans-2-decalols as inhibitors of norepinephrine N-methyltransferase. | J Med Chem 25: 1250-2 (1983) | TBA | 2D 3D TSV |
7143366 | 19 | Probes of the active site of norepinephrine N-methyltransferase: effect of hydrophobic and hydrophilic interactions on side-chain binding of amphetamine and alpha-methylbenzylamine. | J Med Chem 25: 1248-50 (1983) | TBA | 2D 3D TSV |
7143361 | 6 | Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin. | J Med Chem 25: 1227-30 (1983) | TBA | 2D 3D TSV |
7143357 | 6 | Directional probes of the hydrophobic component of the aromatic ring binding site of norepinephrine N-methyltransferase. | J Med Chem 25: 1204-8 (1983) | TBA | 2D 3D TSV |
7143356 | 17 | Importance of the aromatic ring in adrenergic amines. 7. Comparison of the stereoselectivity of norepinephrine N-methyltransferase for aromatic vs. nonaromatic substrates and inhibitors. | J Med Chem 25: 1198-204 (1983) | TBA | 2D 3D TSV |
7143354 | 25 | Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives. | J Med Chem 25: 1184-8 (1983) | TBA | 2D 3D TSV |
7120288 | 12 | Aporphines. 39. Synthesis, dopamine receptor binding, and pharmacological activity of (R)-(-)- and (S)-(+)-2-hydroxyapomorphine. | J Med Chem 25: 990-2 (1982) | TBA | 2D 3D TSV |
7120280 | 9 | Structure-activity relationships in potentially hallucinogenic N,N-dialkyltryptamines substituted in the benzene moiety. | J Med Chem 25: 908-13 (1982) | TBA | 2D 3D TSV |
7120277 | 82 | Inhibition of rat hepatic microsomal aminopyrine N-demethylase activity by benzimidazole derivatives. Quantitative structure-activity relationships. | J Med Chem 25: 887-92 (1982) | TBA | 2D 3D TSV |
7109844 | 11 | The binding of [3H]nitrendipine to receptors for calcium channel antagonists in the heart, cerebral cortex, and ileum of rats. | Life Sci 30: 2191-202 (1982) | University of Arizona | 2D 3D TSV |
7108907 | 11 | 10-Propargylaminopterin and alkyl homologues of methotrexate as inhibitors of folate metabolism. | J Med Chem 25: 877-80 (1982) | TBA | 2D 3D TSV |
7108902 | 18 | Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain. | J Med Chem 25: 855-8 (1982) | TBA | 2D 3D TSV |
7108901 | 2 | Synthesis and dopamine receptor binding of exo- and endo-2-amino-6,7-dihydroxybenzonorbornene, rigid analogues of 2-amino-6,7-dihydroxytetrahydronaphthalene. | J Med Chem 25: 850-4 (1982) | TBA | 2D 3D TSV |
7108896 | 7 | Species- or isozyme-specific enzyme inhibitors. 6. Synthesis and evaluation of two-substrate condensation products as inhibitors of hexokinases and thymidine kinases. | J Med Chem 25: 801-5 (1982) | TBA | 2D 3D TSV |
7097717 | 44 | Species- or isozyme-specific enzyme inhibitors. 5. Differential effects of thymidine substituents on affinity for rat thymidine kinase isozymes. | J Med Chem 25: 644-9 (1982) | TBA | 2D 3D TSV |
7097715 | 37 | Inhibitors of hepatic mixed-function oxidases. 4. Effects of benzimidazole and related compounds on aryl hydrocarbon hydroxylase activity from phenobarbitone and 3-methylcholanthrene induced rats. | J Med Chem 25: 622-6 (1982) | TBA | 2D 3D TSV |
7086847 | 4 | Inhibitors of adenosine deaminase. Studies in combining high-affinity enzyme-binding structural units. erythro-1,6-Dihydro-6-(hydroxymethyl)-9-(2-hydroxy-3-nonyl)purine and erythro-9-(2-hydroxy-3-nonyl)purine. | J Med Chem 25: 603-5 (1982) | TBA | 2D 3D TSV |
7086841 | 18 | Synthesis and biochemical properties of chemically stable product analogues of the reaction catalyzed by S-adenosyl-L-methionine decarboxylase. | J Med Chem 25: 550-6 (1982) | TBA | 2D 3D TSV |
7086836 | 1 | Inhibition by 5-(substituted-benzyl)-2,4-diaminopyrimidines of murine tumor (L5178Y) cell cultures sensitive to and resistant to methotrexate. Further evidence for the sensitivity of resistant cells to hydrophobic drugs. | J Med Chem 25: 518-22 (1982) | TBA | 2D 3D TSV |
7086824 | 15 | 2,3-dihydro and carbocyclic analogues of tryptamines: interaction with serotonin receptors. | J Med Chem 25: 68-70 (1982) | TBA | 2D 3D TSV |
7086823 | 46 | 4-hydroxyquinoline-3-carboxylic acids as inhibitors of cell respiration. 2. Quantitative structure-activity relationship of dehydrogenase enzyme and Ehrlich ascites tumor cell inhibitions. | J Med Chem 25: 57-63 (1982) | TBA | 2D 3D TSV |
7069726 | 7 | Lysine and ornithine analogues of methotrexate as inhibitors of dihydrofolate reductase. | J Med Chem 25: 475-7 (1982) | TBA | 2D 3D TSV |
7069722 | 167 | A comparison of the inhibitory action of 5-(substituted-benzyl)-2,4-diaminopyrimidines on dihydrofolate reductase from chicken liver with that from bovine liver. | J Med Chem 25: 435-40 (1982) | TBA | 2D 3D TSV |
7069721 | 2 | Molecular structures of 2,4-diaminopyrimidine antifolates with antineoplastic activity. | J Med Chem 25: 427-30 (1982) | TBA | 2D 3D TSV |
7069705 | 5 | Catechol O-methyltransferase. 12. Affinity labeling the active site with the oxidation products of 5,6-dihydroxyindole. | J Med Chem 25: 263-71 (1982) | TBA | 2D 3D TSV |
7057425 | 13 | Syntheses of alpha- and gamma-substituted amides, peptides, and esters of methotrexate and their evaluation as inhibitors of folate metabolism. | J Med Chem 25: 182-7 (1982) | TBA | 2D 3D TSV |
7045370 | 8 | Renin inhibitors. Substitution of the leucyl residues of Leu-Leu-Val-Phe-OCH3 with 3-amino-2-hydroxy-5-methylhexanoic acid. | J Med Chem 25: 605-10 (1982) | TBA | 2D 3D TSV |
7035668 | 65 | 2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 5. 3',5'-Dimethoxy-4'-substituted-benzyl analogues of trimethoprim. | J Med Chem 24: 933-41 (1982) | TBA | 2D 3D TSV |
7017146 | 72 | Quantitative structure-selectivity relationships. Comparison of the inhibition of Escherichia coli and bovine liver dihydrofolate reductase by 5-(substituted-benzyl)-2,4-diaminopyrimidines. | J Med Chem 24: 538-44 (1981) | TBA | 2D 3D TSV |