Search by PubMed Identification
PMID | Data | Article Title | Citation | Organization | Data Download |
---|---|---|---|---|---|
8997630 | 77 | Iloperidone binding to human and rat dopamine and 5-HT receptors. | Eur J Pharmacol 317: 417-23 (1996) | Hoechst Marion Roussel Inc | 2D 3D TSV |
8996189 | 24 | Cloning, expression and pharmacological characterization of rabbit adenosine A1 and A3 receptors. | J Pharmacol Exp Ther 280: 122-8 (1997) | Pfizer Inc | 2D 3D TSV |
8996185 | 121 | Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. | J Pharmacol Exp Ther 280: 83-97 (1997) | Synthélabo Recherche | 2D 3D TSV |
8988595 | 5 | Bastadin 20 and bastadin O-sulfate esters from Ianthella basta: novel modulators of the Ry1R FKBP12 receptor complex. | J Nat Prod 59: 1121-7 (1997) | University of California | 2D 3D TSV |
8984162 | 3 | Two fungal lanostane derivatives as phospholipase A2 inhibitors. | J Nat Prod 59: 977-9 (1997) | Universitat de Val£ncia | 2D 3D TSV |
8978857 | 17 | Structure-activity relationships of phomactin derivatives as platelet activating factor antagonists. | J Med Chem 39: 5281-4 (1997) | Sankyo Co., Ltd | 2D 3D TSV |
8978855 | 16 | Synthesis and bioactivity of novel bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships and increased metabolic stability of novel substituted pyridine analogs. | J Med Chem 39: 5267-75 (1997) | Pharmacia & Upjohn | 2D 3D TSV |
8978853 | 57 | Genetic neural networks for quantitative structure-activity relationships: improvements and application of benzodiazepine affinity for benzodiazepine/GABAA receptors. | J Med Chem 39: 5246-56 (1997) | Harvard University | 2D 3D TSV |
8978852 | 10 | Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent. | J Med Chem 39: 5236-45 (1997) | Glaxo Wellcome Research and Development | 2D 3D TSV |
8978850 | 205 | Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A. | J Med Chem 39: 5215-27 (1996) | Sphinx Laboratories | 2D 3D TSV |
8978846 | 68 | Synthesis and phospholipase A2 inhibitory activity of thielocin B3 derivatives. | J Med Chem 39: 5183-91 (1997) | Shionogi & Co., Ltd | 2D 3D TSV |
8978844 | 86 | Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides. | J Med Chem 39: 5159-75 (1997) | Eli Lilly and Company | 2D 3D TSV |
8978843 | 119 | Indole inhibitors of human nonpancreatic secretory phospholipase A2. 2. Indole-3-acetamides with additional functionality. | J Med Chem 39: 5137-58 (1997) | Eli Lilly and Company | 2D 3D TSV |
8978842 | 9 | Synthesis and evaluation of two positron-labeled nitric oxide synthase inhibitors, S-[11C]methylisothiourea and S-(2-[18F]fluoroethyl)isothiourea, as potential positron emission tomography tracers. | J Med Chem 39: 5110-8 (1997) | Washington University | 2D 3D TSV |
8978840 | 12 | Synthesis and bioevaluation of delta 7-5-desaturase inhibitors, an enzyme late in the biosynthesis of the fungal sterol ergosterol. | J Med Chem 39: 5092-9 (1997) | Institute | 2D 3D TSV |
8978838 | 24 | Design, synthesis, and evaluation of nonpeptidic inhibitors of human rhinovirus 3C protease. | J Med Chem 39: 5072-82 (1997) | Agouron Pharmaceuticals Inc | 2D 3D TSV |
8978837 | 60 | Structure-based alignment and comparative molecular field analysis of acetylcholinesterase inhibitors. | J Med Chem 39: 5064-71 (1997) | University of North Carolina | 2D 3D TSV |
8978835 | 18 | Indole derivatives as a new class of steroid 5 alpha-reductase inhibitors. | J Med Chem 39: 5047-52 (1997) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
8978834 | 33 | Bicyclic N-hydroxyurea inhibitors of 5-lipoxygenase: pharmacodynamic, pharmacokinetic, and in vitro metabolic studies characterizing N-hydroxy-N-(2,3-dihydro-6-(phenylmethoxy)-3-benzofuranyl)urea. | J Med Chem 39: 5035-46 (1997) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8978832 | 18 | Identification of retinoic acid receptor beta subtype specific agonists. | J Med Chem 39: 5027-30 (1997) | Allergan Inc | 2D 3D TSV |
8968364 | 10 | Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist. | J Pharmacol Exp Ther 279: 1392-403 (1996) | Pharmacia and Upjohn, Inc. | 2D 3D TSV |
8968358 | 12 | The interaction of the enantiomers of aceclidine with subtypes of the muscarinic receptor. | J Pharmacol Exp Ther 279: 1335-44 (1996) | University of California | 2D 3D TSV |
8960563 | 12 | Quantitative structure-activity relationship study of fibrinogen inhibitors, [[4-(4-amidinophenoxy)butanoyl]aspartyl]valine (FK633) derivatives, using a novel hydrophobic descriptor. | J Med Chem 39: 5017-20 (1997) | Fujisawa Pharmaceutical Company, Ltd | 2D 3D TSV |
8960557 | 27 | Synthesis, biological activity, and molecular modeling of selective 5-HT(2C/2B) receptor antagonists. | J Med Chem 39: 4966-77 (1997) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8960555 | 13 | Potent 6-desfluoro-8-methylquinolones as new lead compounds in antibacterial chemotherapy. | J Med Chem 39: 4952-7 (1996) | Universit£ di Perugia | 2D 3D TSV |
8960554 | 30 | Analogues of capsaicin with agonist activity as novel analgesic agents: structure-activity studies. 4. Potent, orally active analgesics. | J Med Chem 39: 4942-51 (1996) | Sandoz Institute for Medical Research | 2D 3D TSV |
8960553 | 60 | Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter. | J Med Chem 39: 4935-41 (1997) | Drew University | 2D 3D TSV |
8960552 | 58 | Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4. | J Med Chem 39: 4928-34 (1997) | Universit£ di Bari | 2D 3D TSV |
8960551 | 74 | Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists. | J Med Chem 39: 4920-7 (1997) | Centre de Recherche Pierre Fabre | 2D 3D TSV |
8960550 | 5 | Conformationally constrained analogues of diacylglycerol. 13. Protein kinase C ligands based on templates derived from 2,3-dideoxy-L-erythro(threo)-hexono-1,4-lactone and 2-deoxyapiolactone. | J Med Chem 39: 4912-9 (1997) | National Cancer Institute-Bethesda | 2D 3D TSV |
8960549 | 19 | Tyrphostins. 6. Dimeric benzylidenemalononitrile tyrophostins: potent inhibitors of EGF receptor tyrosine kinase in vitro. | J Med Chem 39: 4905-11 (1996) | Hebrew University of Jerusalem | 2D 3D TSV |
8960547 | 19 | Anti-inflammatory 17beta-thioalkyl-16alpha,17alpha-ketal and -acetal androstanes: a new class of airway selective steroids for the treatment of asthma. | J Med Chem 39: 4888-96 (1997) | Rh£ne-Poulenc Rorer Central Research | 2D 3D TSV |
8960546 | 160 | Development of potent thrombin receptor antagonist peptides. | J Med Chem 39: 4879-87 (1997) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8960545 | 21 | (Carboxyalkyl)benzyl propargyl ethers as selective inhibitors of leukocyte-type 12-lipoxygenases. | J Med Chem 39: 4871-8 (1997) | Wayne State University | 2D 3D TSV |
8960544 | 10 | Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists. | J Med Chem 39: 4867-70 (1997) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8960059 | 1 | Reversal of P-glycoprotein-associated multidrug resistance by ivermectin. | Biochem Pharmacol 53: 17-25 (1997) | Institute of Parasitology of McGill University | 2D 3D TSV |
8956326 | 4 | Human dipeptide transporter, hPEPT1, stably transfected into Chinese hamster ovary cells. | Pharm Res 13: 1631-4 (1996) | University of California San Francisco | 2D 3D TSV |
8955089 | 4 | Role of salt bridge formation in antigen-antibody interaction. Entropic contribution to the complex between hen egg white lysozyme and its monoclonal antibody HyHEL10. | J Biol Chem 271: 32612-6 (1996) | Tohoku University | 2D 3D TSV |
8946946 | 32 | Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor. | FEBS Lett 398: 19-25 (1996) | CNRS UPR 9023 | 2D 3D TSV |
8946748 | 2 | Six lignans from Phyllanthus myrtifolius. | J Nat Prod 59: 1061-5 (1996) | National Taiwan University | 2D 3D TSV |
8941400 | 12 | Nudicauline and elatine as potent norditerpenoid ligands at rat neuronal alpha-bungarotoxin binding sites: importance of the 2-(methylsuccinimido)benzoyl moiety for neuronal nicotinic acetylcholine receptor binding. | J Med Chem 39: 4860-6 (1997) | School of Pharmacy and Pharmacology | 2D 3D TSV |
8941399 | 7 | Estrogenic triarylethylene acetic acids: effect of structural variation on estrogen receptor affinity and estrogenic potency and efficacy in MCF-7 cells. | J Med Chem 39: 4853-9 (1996) | University of Georgia | 2D 3D TSV |
8941398 | 17 | Synthesis and biological activity of conformationally restricted analogs of milnacipran: (1S,2R)-1-phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxami de, an efficient noncompetitive N-methyl-D-aspartic acid receptor antagonist. | J Med Chem 39: 4844-52 (1997) | Hokkaido University | 2D 3D TSV |
8941396 | 20 | Solution of the conformation and alignment tensors for the binding of trimethoprim and its analogs to dihydrofolate reductase: 3D-quantitative structure-activity relationship study using molecular shape analysis, 3-way partial least-squares regression, and 3-way factor analysis. | J Med Chem 39: 4825-32 (1996) | University of Illinois at Chicago 60612 | 2D 3D TSV |
8941387 | 10 | Synthesis and dopamine transporter affinity of 2-(methoxycarbonyl)-9-methyl-3-phenyl-9-azabicyclo[3.3.1]nonane derivatives. | J Med Chem 39: 4744-9 (1997) | University of New Orleans | 2D 3D TSV |
8941385 | 18 | Understanding the binding of 5-substituted 2'-deoxyuridine substrates to thymidine kinase of herpes simplex virus type-1. | J Med Chem 39: 4727-37 (1997) | Katholieke Universiteit Leuven | 2D 3D TSV |
8941384 | 51 | 5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates. | J Med Chem 39: 4717-26 (1997) | University of Groningen | 2D 3D TSV |
8941383 | 146 | Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909). | J Med Chem 39: 4704-16 (1997) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8941382 | 40 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. | J Med Chem 39: 4692-703 (1997) | Glaxo Wellcome Inc. | 2D 3D TSV |
8935801 | 586 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. | Psychopharmacology (Berl) 124: 57-73 (1996) | Janssen Research Foundation | 2D 3D TSV |
8930187 | 5 | Pharmacokinetic/pharmacodynamic relationship of benzodiazepines in the direct cortical stimulation model of anticonvulsant effect. | J Pharmacol Exp Ther 279: 803-12 (1996) | Leiden University | 2D 3D TSV |
8917655 | 72 | 6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists. | J Med Chem 39: 4667-75 (1996) | National Institute of Diabetes | 2D 3D TSV |
8917654 | 7 | High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines. | J Med Chem 39: 4654-66 (1996) | Upjohn Laboratories | 2D 3D TSV |
8917652 | 23 | Structure-based design of HIV protease inhibitors: 5,6-dihydro-4-hydroxy-2-pyrones as effective, nonpeptidic inhibitors. | J Med Chem 39: 4630-42 (1996) | Pharmacia & Upjohn | 2D 3D TSV |
8917650 | 140 | Synthesis, structure-activity relationships, and pharmacokinetic properties of dihydroorotate dehydrogenase inhibitors: 2-cyano-3-cyclopropyl-3-hydroxy-N-[3'-methyl-4'-(trifluoromethyl)phenyl ] propenamide and related compounds. | J Med Chem 39: 4608-21 (1996) | Hoechst Marion Roussel Inc | 2D 3D TSV |
8917649 | 60 | Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist. | J Med Chem 39: 4602-7 (1996) | University of Camerino | 2D 3D TSV |
8917645 | 20 | Synthesis and biological activity of aromatic amino acid phosphoramidates of 5-fluoro-2'-deoxyuridine and 1-beta-arabinofuranosylcytosine: evidence of phosphoramidase activity. | J Med Chem 39: 4569-75 (1996) | University of Minnesota | 2D 3D TSV |
8917644 | 49 | 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase. | J Med Chem 39: 4563-8 (1996) | Duquesne University | 2D 3D TSV |
8917642 | 4 | Studies on selectin blocker. 3. Investigation of the carbohydrate ligand sialyl Lewis X recognition site of P-selectin. | J Med Chem 39: 4547-53 (1996) | Kanebo Ltd. | 2D 3D TSV |
8917639 | 50 | Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties. | J Med Chem 39: 4531-6 (1996) | Corvas International Inc | 2D 3D TSV |
8917638 | 26 | Potent and selective thrombin inhibitors incorporating the constrained arginine mimic l-3-piperidyl(N-guanidino)alanine at P1. | J Med Chem 39: 4527-30 (1996) | Corvas International Inc | 2D 3D TSV |
8910390 | 13 | Molecular and pharmacological characterization of native cortical gamma-aminobutyric acidA receptors containing both alpha1 and alpha3 subunits. | J Biol Chem 271: 27902-11 (1996) | Universidad de Sevilla | 2D 3D TSV |
8910290 | 5 | Inactivation of a novel neuropeptide Y/peptide YY receptor gene in primate species. | J Biol Chem 271: 27217-20 (1996) | Yamanouchi Pharmaceutical Co., Ltd | 2D 3D TSV |
8904845 | 3 | Isolation and structure of leukotriene-A4 hydrolase inhibitor: 8(S)-amino-2(R)-methyl-7-oxononanoic acid produced by Streptomyces diastaticus. | J Nat Prod 59: 962-4 (1997) | Searle Research and Development | 2D 3D TSV |
8903934 | 7 | Pharmacological and functional characterisation of the wild-type and site-directed mutants of the human H1 histamine receptor stably expressed in CHO cells. | J Recept Signal Transduct Res 15: 91-102 (1995) | Universite Libre de Bruxelles | 2D 3D TSV |
8903510 | 9 | Peripheral 5-HT4 receptors. | FASEB J 10: 1398-407 (1996) | Roche Bioscience | 2D 3D TSV |
8894098 | 20 | Discovery and optimization of nonpeptide HIV-1 protease inhibitors. | Bioorg Med Chem 4: 1401-10 (1996) | Parke-Davis Pharmaceutical Research | 2D 3D TSV |
8893849 | 10 | Synthesis and solution conformation of cyclo[RGDRGD]: a cyclic peptide with selectivity for the alpha V beta 3 receptor. | J Med Chem 39: 4520-6 (1996) | Texas A&M University | 2D 3D TSV |
8893848 | 21 | Head group analogs of arachidonylethanolamide, the endogenous cannabinoid ligand. | J Med Chem 39: 4515-9 (1996) | University of Connecticut | 2D 3D TSV |
8893842 | 6 | Aspartic acid conjugates of 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1(3-aminophenyl)-2-(1-pyrrolidi nyl) ethyl]acetamide: kappa opioid receptor agonists with limited access to the central nervous system. | J Med Chem 39: 4478-82 (1996) | University of Minnesota | 2D 3D TSV |
8893841 | 23 | Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties. | J Med Chem 39: 4471-7 (1996) | Université Blaise Pascal | 2D 3D TSV |
8893840 | 12 | The simulated binding of (+/-)-2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]meth yl] -1H-inden-1-one hydrochloride (E2020) and related inhibitors to free and acylated acetylcholinesterases and corresponding structure-activity analyses. | J Med Chem 39: 4460-70 (1996) | Eisai Co., Ltd | 2D 3D TSV |
8893838 | 106 | Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist. | J Med Chem 39: 4439-50 (1996) | Universidad Complutense | 2D 3D TSV |
8893836 | 50 | Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists. | J Med Chem 39: 4421-9 (1996) | Uppsala University | 2D 3D TSV |
8893834 | 30 | Synthesis, activity, and molecular modeling of a new series of tricyclic pyridazinones as selective aldose reductase inhibitors. | J Med Chem 39: 4396-405 (1996) | TBA | 2D 3D TSV |
8893833 | 42 | Heterocyclic ureas: inhibitors of acyl-CoA:cholesterol O-acyltransferase as hypocholesterolemic agents. | J Med Chem 39: 4382-95 (1996) | Warner-Lambert Company | 2D 3D TSV |
8893829 | 13 | Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 receptor antagonists. | J Med Chem 39: 4358-60 (1996) | Neurocrine Biosciences Inc | 2D 3D TSV |
8893828 | 28 | Rapid microscale synthesis, a new method for lead optimization using robotics and solution phase chemistry: application to the synthesis and optimization of corticotropin-releasing factor1 receptor antagonists. | J Med Chem 39: 4354-7 (1996) | Neurocrine Biosciences Inc | 2D 3D TSV |
8893827 | 17 | Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors. | J Med Chem 39: 4349-53 (1996) | Upjohn | 2D 3D TSV |
8891613 | 25 | Characterisation of the specific binding of the histamine H3 receptor antagonist radioligand [3H]GR168320. | Eur J Pharmacol 311: 305-10 (1996) | Glaxo Research & Development Ltd. | 2D 3D TSV |
8889190 | 55 | Thermodynamics of hydrogen bond and hydrophobic interactions in cyclodextrin complexes. | Biophys J 71: 2144-54 (1996) | NIH | 2D 3D TSV |
8887981 | 72 | A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand. | Neuropharmacology 35: 725-34 (1996) | Abbott Laboratories | 2D 3D TSV |
8884876 | 47 | Characterisation of the melanocortin 4 receptor by radioligand binding. | Pharmacol Toxicol 79: 161-5 (1996) | Uppsala University | 2D 3D TSV |
8882431 | 4 | Antineoplastic agents. 340. Isolation and structural elucidation of bryostatins 16-18. | J Nat Prod 59: 286-9 (1997) | Arizona State University | 2D 3D TSV |
8879560 | 22 | Structure-activity relationships of HIV-1 PR inhibitors containing AHPBA--II. Modification of pyrrolidine ring at P1' proline. | Bioorg Med Chem 4: 1365-77 (1996) | Sankyo Co., Ltd | 2D 3D TSV |
8879541 | 35 | Tyrphostins IV--highly potent inhibitors of EGF receptor kinase. Structure-activity relationship study of 4-anilidoquinazolines. | Bioorg Med Chem 4: 1203-7 (1996) | Hebrew University of Jerusalem | 2D 3D TSV |
8878062 | 8 | Transport of small organic cations in the rat liver. The role of the organic cation transporter OCT1. | Naunyn Schmiedebergs Arch Pharmacol 354: 320-6 (1997) | University of Heidelberg | 2D 3D TSV |
8876023 | 52 | Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor. | Psychopharmacology (Berl) 126: 234-40 (1996) | University of Turku | 2D 3D TSV |
8867105 | 49 | Pharmacological comparison between [3H]GR 113808 binding sites and functional 5-HT4 receptors in neurons. | Eur J Pharmacol 298: 165-74 (1996) | CNRS UPR 9023 | 2D 3D TSV |
8864237 | 4 | Specific inhibition of human immunodeficiency virus type 1 reverse transcriptase mediated by soulattrolide, a coumarin isolated from the latex of calophyllum teysmannii. | J Nat Prod 59: 839-42 (1997) | Chulalongkorn University | 2D 3D TSV |
8863838 | 28 | Coupling of metabotropic glutamate receptors 2 and 4 to G alpha 15, G alpha 16, and chimeric G alpha q/i proteins: characterization of new antagonists. | Mol Pharmacol 50: 923-30 (1996) | UPR Centre | 2D 3D TSV |
8863817 | 4 | Structural determinants of substrates for the prostaglandin transporter PGT. | Mol Pharmacol 50: 738-42 (1996) | Albert Einstein College of Medicine | 2D 3D TSV |
8863814 | 21 | Identification and characterization of novel somatostatin antagonists. | Mol Pharmacol 50: 709-15 (1996) | Cyenamid Agricultural Research Center | 2D 3D TSV |
8863812 | 8 | Design and synthesis of histidine analogues of folic acid and methotrexate as potential folylpolyglutamate synthetase inhibitors. | J Med Chem 39: 4340-4 (1996) | State University of New York | 2D 3D TSV |
8863811 | 56 | Synthesis and evaluation of pregnane derivatives as inhibitors of human testicular 17 alpha-hydroxylase/C17,20-lyase. | J Med Chem 39: 4335-9 (1996) | University of Maryland | 2D 3D TSV |
8863807 | 71 | HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis. | J Med Chem 39: 4299-312 (1996) | DuPont Pharmaceuticals Company | 2D 3D TSV |
8863806 | 68 | 3-amino-3,4-dihydro-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 2. Synthesis and quantitative structure-activity relationship studies of spiro[pyrrolidine- and piperidine-2,3'(2'H)-benzopyrans] | J Med Chem 39: 4285-98 (1996) | Université d'Orléans | 2D 3D TSV |
8863805 | 35 | Molecular basis of peripheral vs central benzodiazepine receptor selectivity in a new class of peripheral benzodiazepine receptor ligands related to alpidem. | J Med Chem 39: 4275-84 (1996) | Università di Siena | 2D 3D TSV |
8863804 | 141 | Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs. | J Med Chem 39: 4261-74 (1996) | Eli Lilly and Company | 2D 3D TSV |
8863803 | 22 | Novel potent sigma 1 ligands: N-[omega-(tetralin-1-yl)alkyl]piperidine derivatives. | J Med Chem 39: 4255-60 (1996) | Universit£ di Bari | 2D 3D TSV |
8863801 | 40 | Synthesis, resolution, and preliminary evaluation of trans-2-amino-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes and related derivatives as dopamine receptors ligands. | J Med Chem 39: 4238-46 (1996) | Universit£ di Camerino | 2D 3D TSV |
8863800 | 115 | Affinity for dopamine D2, D3, and D4 receptors of 2-aminotetralins. Relevance of D2 agonist binding for determination of receptor subtype selectivity. | J Med Chem 39: 4233-7 (1996) | University of Groningen | 2D 3D TSV |
8863798 | 52 | 2-alkenyl and 2-alkyl derivatives of adenosine and adenosine-5'-N-ethyluronamide: different affinity and selectivity of E- and Z-diastereomers at A2A adenosine receptors. | J Med Chem 39: 4211-7 (1996) | Universit£ di Camerino | 2D 3D TSV |
8863797 | 9 | Hydroxamic acid-based bisubstrate analog inhibitors of Ras farnesyl protein transferase. | J Med Chem 39: 4197-210 (1996) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8863796 | 65 | Structure-activity relationships for inhibition of inosine monophosphate dehydrogenase by nuclear variants of mycophenolic acid. | J Med Chem 39: 4181-96 (1996) | Syntex Research | 2D 3D TSV |
8863795 | 24 | Peptidomimetic inhibitors of herpes simplex virus ribonucleotide reductase with improved in vivo antiviral activity. | J Med Chem 39: 4173-80 (1996) | Bio-M£ga/Boehringer Ingelheim Research Inc. | 2D 3D TSV |
8863793 | 14 | Inactivation of S-adenosyl-L-homocysteine hydrolase by amide and ester derivatives of adenosine-5'-carboxylic acid. | J Med Chem 39: 4162-6 (1996) | Brigham Young University | 2D 3D TSV |
8863792 | 22 | Synthesis and structure-activity relationship of pyrazolo[3,4-d]pyrimidines: potent and selective adenosine A1 receptor antagonists. | J Med Chem 39: 4156-61 (1996) | Griffith University | 2D 3D TSV |
8863790 | 55 | Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. | J Med Chem 39: 4142-8 (1996) | National Institute of Diabetes | 2D 3D TSV |
8863789 | 31 | 3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine transporter. | J Med Chem 39: 4139-41 (1996) | Research Triangle Institute | 2D 3D TSV |
8862725 | 8 | Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay. | Anticancer Drugs 7: 568-78 (1997) | Strasbourg 1 University | 2D 3D TSV |
8845011 | 25 | A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines. | Life Sci 59: 1259-68 (1996) | Eli Lilly and Company | 2D 3D TSV |
8831779 | 22 | Cycloalkylpyranones and cycloalkyldihydropyrones as HIV protease inhibitors: exploring the impact of ring size on structure-activity relationships. | J Med Chem 39: 4125-30 (1996) | Pharmacia and Upjohn, Inc. | 2D 3D TSV |
8831778 | 22 | The use of topographical constraints in receptor mapping: investigation of the topographical requirements of the tryptophan 30 residue for receptor binding of Asp-Tyr-D-Phe-Gly-Trp-(N-Me)Nle-Asp-Phe-NH2 (SNF 9007), a cholecystokinin (26-33) analogue that binds to both CCK-B and delta-opioid recepto | J Med Chem 39: 4120-4 (1996) | University of Arizona | 2D 3D TSV |
8831777 | 48 | Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist. | J Med Chem 39: 4116-9 (1996) | Abbott Laboratories | 2D 3D TSV |
8831775 | 34 | New purines and purine analogs as modulators of multidrug resistance. | J Med Chem 39: 4099-108 (1996) | Institut de Recherches Servier | 2D 3D TSV |
8831774 | 261 | Novel peptidyl alpha-keto amide inhibitors of calpains and other cysteine proteases. | J Med Chem 39: 4089-98 (1996) | Georgia Institute of Technology | 2D 3D TSV |
8831772 | 18 | Principal components describing biological activities and molecular diversity of heterocyclic aromatic ring fragments. | J Med Chem 39: 4065-72 (1996) | Organon Research and Development Group | 2D 3D TSV |
8831771 | 64 | On the bioisosteric potential of diazines: diazine analogues of the combined thromboxane A2 receptor antagonist and synthetase inhibitor Ridogrel. | J Med Chem 39: 4058-64 (1996) | University of Innsbruck | 2D 3D TSV |
8831770 | 136 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. | J Med Chem 39: 4044-57 (1996) | Hoechst Marion Roussel Inc | 2D 3D TSV |
8831769 | 42 | Derivatives of (R)- and (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: synthesis and interactions with 5-HT1A receptors. | J Med Chem 39: 4036-43 (1996) | Uppsala University | 2D 3D TSV |
8831768 | 65 | Synthesis and transporter binding properties of 3 beta-(4'-alkyl-, 4'-alkenyl-, and 4'-alkynylphenyl)nortropane-2 beta-carboxylic acid methyl esters: serotonin transporter selective analogs. | J Med Chem 39: 4027-35 (1996) | Research Triangle Institute | 2D 3D TSV |
8831767 | 60 | Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors. | J Med Chem 39: 4017-26 (1996) | Virginia Commonwealth University | 2D 3D TSV |
8831765 | 9 | Homology modeling of metabotropic glutamate receptors. (mGluRs) structural motifs affecting binding modes and pharmacological profile of mGluR1 agonists and competitive antagonists. | J Med Chem 39: 3998-4006 (1996) | Università di Perugia | 2D 3D TSV |
8831762 | 3 | Novel AMPA receptor antagonists: synthesis and structure-activity relationships of 1-hydroxy-7-(1H-imidazol-1-yl)-6-nitro-2,3(1H,4H)- quinoxalinedione and related compounds. | J Med Chem 39: 3971-9 (1996) | Yamanouchi Pharmaceutical Company Limited | 2D 3D TSV |
8831761 | 53 | Dioxabicyclooctanyl naphthalenenitriles as nonredox 5-lipoxygenase inhibitors: structure-activity relationship study directed toward the improvement of metabolic stability. | J Med Chem 39: 3951-70 (1996) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
8831760 | 108 | 5-Lipoxygenase inhibitors: synthesis and structure-activity relationships of a series of 1-aryl-2H,4H-tetrahydro-1,2,4-triazin-3-ones. | J Med Chem 39: 3938-50 (1996) | Abbott Laboratories | 2D 3D TSV |
8831759 | 16 | 1-substituted 4-aryl-5-pyridinylimidazoles: a new class of cytokine suppressive drugs with low 5-lipoxygenase and cyclooxygenase inhibitory potency. | J Med Chem 39: 3929-37 (1996) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8831757 | 16 | Heterocyclic amides: inhibitors of acyl-CoA:cholesterol O-acyl transferase with hypocholesterolemic activity in several species and antiatherosclerotic activity in the rabbit. | J Med Chem 39: 3908-19 (1996) | Warner-Lambert Company | 2D 3D TSV |
8831752 | 9 | Synthesis and pharmacology of a very potent cannabinoid lacking a phenolic hydroxyl with high affinity for the CB2 receptor. | J Med Chem 39: 3875-7 (1996) | Clemson University | 2D 3D TSV |
8824284 | 43 | Identification of a novel hypothalamic neuropeptide Y receptor associated with feeding behavior. | J Biol Chem 271: 26315-9 (1996) | Bayer Corporation | 2D 3D TSV |
8824261 | 8 | Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity. | J Biol Chem 271: 26157-64 (1996) | Institute for Biochemistry | 2D 3D TSV |
8822531 | 111 | Radioreceptor binding profile of the atypical antipsychotic olanzapine. | Neuropsychopharmacology 14: 87-96 (1996) | Eli Lilly and Company | 2D 3D TSV |
8821530 | 16 | In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties. | Br J Pharmacol 117: 427-434 (1996) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8818233 | 18 | 5H-pyrrolo[1,2-b] [1,2,5]benzothiadiazepines (PBTDs): a novel class of non-nucleoside reverse transcriptase inhibitors. | Bioorg Med Chem 4: 837-50 (1996) | Sapienza University of Rome | 2D 3D TSV |
8813606 | 15 | [3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor. | Eur J Pharmacol 304: 231-5 (1996) | Synaptic Pharmaceutical Corporation | 2D 3D TSV |
8813598 | 34 | Affinity of various ligands for GABAA receptors containing alpha 4 beta 3 gamma 2, alpha 4 gamma 2, or alpha 1 beta 3 gamma 2 subunits. | Eur J Pharmacol 304: 155-62 (1996) | University Clinic for Psychiatry | 2D 3D TSV |
8809171 | 13 | (E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity. | J Med Chem 39: 3837-41 (1996) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8809168 | 31 | A novel series of (phenoxyalkyl)imidazoles as potent H3-receptor histamine antagonists. | J Med Chem 39: 3806-13 (1996) | University College London | 2D 3D TSV |
8809166 | 10 | Unsaturated side chain beta-11-hydroxyhexahydrocannabinol analogs. | J Med Chem 39: 3790-6 (1996) | University of Hawaii | 2D 3D TSV |
8809165 | 120 | Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors. | J Med Chem 39: 3769-89 (1996) | Upjohn | 2D 3D TSV |
8809164 | 5 | Structure-activity relationships study of two series of leukotriene B4 antagonists: novel indolyl and naphthyl compounds substituted with a 2-[methyl(2-phenethyl)amino]-2-oxoethyl side chain. | J Med Chem 39: 3756-68 (1996) | Rhône-Poulenc Rorer | 2D 3D TSV |
8809163 | 3 | A novel series of [2-[methyl(2-phenethyl)amino]-2-oxoethyl] benzene-containing leukotriene B4 antagonists: initial structure-activity relationships. | J Med Chem 39: 3748-55 (1996) | Rhone-Poulenc Rorer Central Research | 2D 3D TSV |
8809161 | 90 | Serotonin 5-HT2 receptor, dopamine D2 receptor, and alpha 1 adrenoceptor antagonists. Conformationally flexible analogues of the atypical antipsychotic sertindole. | J Med Chem 39: 3723-38 (1996) | H. Lundbeck A/S | 2D 3D TSV |
8809160 | 132 | Design, synthesis, and evaluation of 2 beta-alkenyl penam sulfone acids as inhibitors of beta-lactamases. | J Med Chem 39: 3712-22 (1996) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
8809159 | 26 | Iodinated analogs of trimetoquinol as highly potent and selective beta 2-adrenoceptor ligands. | J Med Chem 39: 3701-11 (1996) | University of Tennessee-Memphis | 2D 3D TSV |
8809156 | 2 | Synthesis and cardiotonic activity of novel pyrimidine derivatives: crystallographic and quantum chemical studies. | J Med Chem 39: 3671-83 (1996) | Università di Padova | 2D 3D TSV |
8809154 | 120 | Potent inhibitors of secretory phospholipase A2: synthesis and inhibitory activities of indolizine and indene derivatives. | J Med Chem 39: 3636-58 (1996) | Shionogi & Co., Ltd | 2D 3D TSV |
8809153 | 60 | Conformationally defined 6-s-trans-retinoic acid analogs. 3. Structure-activity relationships for nuclear receptor binding, transcriptional activity, and cancer chemopreventive activity. | J Med Chem 39: 3625-35 (1996) | University of Alabama at Birmingham | 2D 3D TSV |
8809152 | 65 | Synthesis of a series of aryl kainic acid analogs and evaluation in cells stably expressing the kainate receptor humGluR6. | J Med Chem 39: 3617-24 (1996) | Eli Lilly and Company | 2D 3D TSV |
8798583 | 19 | Highly potent, selective, and low cost bis-tetrahydroaminacrine inhibitors of acetylcholinesterase. Steps toward novel drugs for treating Alzheimer's disease. | J Biol Chem 271: 23646-9 (1996) | Mayo Foundation | 2D 3D TSV |
8788495 | 7 | GR127935: a potent and selective 5-HT1D receptor antagonist. | Behav Brain Res 73: 157-61 (1996) | Glaxo Research and Development Ltd. | 2D 3D TSV |
8788493 | 64 | Novel discriminatory ligands for 5-HT2B receptors. | Behav Brain Res 73: 149-52 (1996) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8784459 | 10 | The chemistry of pseudomonic acid. 17. Dual-action C-1 oxazole derivatives of pseudomonic acid having an extended spectrum of antibacterial activity. | J Med Chem 39: 3596-600 (1996) | SmithKline Beecham Pharmaceuticals | 2D 3D TSV |
8784456 | 55 | ATP-citrate lyase as a target for hypolipidemic intervention. Design and synthesis of 2-substituted butanedioic acids as novel, potent inhibitors of the enzyme. | J Med Chem 39: 3569-84 (1996) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8784455 | 15 | Synthesis and evaluation of aryl-substituted N-(arylethyl)-N-methyl-2-(1-pyrrolidinyl)ethylamines and corresponding arylacetamides for sigma receptor affinity. | J Med Chem 39: 3564-8 (1996) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8784454 | 76 | Synthesis and structure-activity relationships of retinoid X receptor selective diaryl sulfide analogs of retinoic acid. | J Med Chem 39: 3556-63 (1996) | Allergan Inc | 2D 3D TSV |
8784453 | 134 | Orally active, nonpeptide vasopressin V2 receptor antagonists: a novel series of 1-[4-(benzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepines and related compounds. | J Med Chem 39: 3547-55 (1996) | Otsuka Pharmaceutical Co., Ltd | 2D 3D TSV |
8784452 | 11 | Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase. | J Med Chem 39: 3539-46 (1996) | University of Kansas | 2D 3D TSV |
8784451 | 15 | Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist. | J Med Chem 39: 3533-8 (1996) | Allergan Inc | 2D 3D TSV |
8784450 | 73 | Nonlinear quantitative structure-activity relationship for the inhibition of dihydrofolate reductase by pyrimidines. | J Med Chem 39: 3526-32 (1996) | Scripps Research Institute | 2D 3D TSV |
8784449 | 203 | Cyclic HIV protease inhibitors: synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas. | J Med Chem 39: 3514-25 (1996) | DuPont Pharmaceuticals Company | 2D 3D TSV |
8784448 | 63 | 11-substituted (R)-aporphines: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions. | J Med Chem 39: 3503-13 (1996) | Uppsala University | 2D 3D TSV |
8784447 | 63 | 10-substituted 11-oxygenated (R)-aporphines: synthesis, pharmacology, and modeling of 5-HT1A receptor interactions. | J Med Chem 39: 3491-502 (1996) | Uppsala University | 2D 3D TSV |
8784443 | 17 | Novel 5-aminoflavone derivatives as specific antitumor agents in breast cancer. | J Med Chem 39: 3461-9 (1996) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
8784441 | 66 | Synthesis, biological activity, and SARs of pyrrolobenzoxazepine derivatives, a new class of specific"peripheral-type" benzodiazepine receptor ligands. | J Med Chem 39: 3435-50 (1996) | Universit£ di Siena | 2D 3D TSV |
8784440 | 3 | New series of potent, orally bioavailable, non-peptidic cyclic sulfones as HIV-1 protease inhibitors. | J Med Chem 39: 3431-4 (1996) | Gilead Sciences Inc | 2D 3D TSV |
8779894 | 15 | Estradiol 17 beta-D-glucuronide is a high-affinity substrate for oatp organic anion transporter. | Am J Physiol 270: 326-31 (1996) | Albert Einstein College of Medicine | 2D 3D TSV |
8778243 | 1 | Nigranoic acid, a triterpenoid from Schisandra sphaerandra that inhibits HIV-1 reverse transcriptase. | J Nat Prod 59: 525-7 (1996) | Chinese Academy of Sciences | 2D 3D TSV |
8778237 | 2 | HIV inhibitory natural products. 26. Quinoline alkaloids from Euodia roxburghiana. | J Nat Prod 59: 469-71 (1996) | National Cancer Institute | 2D 3D TSV |
8770901 | 16 | Structure-function relationship of the inhibition of the 3,5,3'-triiodothyronine binding to the alpha1- and beta1-thyroid hormone receptor by amiodarone analogs. | Endocrinology 137: 2807-14 (1996) | University of Amsterdam | 2D 3D TSV |
8769372 | 74 | Binding properties of somatostatin receptor subtypes. | Metab Clin Exp 45: 17-20 (1996) | Sandoz Pharma Ltd | 2D 3D TSV |
8765528 | 16 | (+/-)-3-[4'-(N,N-dimethylamino)cinnamyl]benzazepine analogs: novel dopamine D1 receptor antagonists. | J Med Chem 39: 3423-8 (1996) | National Institutes of Health | 2D 3D TSV |
8765520 | 3 | Design, synthesis, and biological evaluation of ellipticine-estradiol conjugates. | J Med Chem 39: 3367-74 (1996) | Purdue University | 2D 3D TSV |
8765519 | 6 | Mechanistic studies on the inactivation of papain by epoxysuccinyl inhibitors. | J Med Chem 39: 3357-66 (1996) | University of Wisconsin | 2D 3D TSV |
8765518 | 17 | New low-density lipoprotein receptor upregulators acting via a novel mechanism. | J Med Chem 39: 3343-56 (1996) | Rhône-Poulenc Rorer | 2D 3D TSV |
8765515 | 37 | 3- and 4-pyridylalkyl adamantanecarboxylates: inhibitors of human cytochrome P450(17 alpha) (17 alpha-hydroxylase/C17,20-lyase). Potential nonsteroidal agents for the treatment of prostatic cancer. | J Med Chem 39: 3319-23 (1996) | Cancer Research Campaign Centre for Cancer Therapeutics | 2D 3D TSV |
8765512 | 25 | Paracyclophanes: a novel class of water-soluble inhibitors of HIV proteinase. | J Med Chem 39: 3291-9 (1996) | Sandoz Research Institute | 2D 3D TSV |
8765511 | 14 | Nonpeptidal P2 ligands for HIV protease inhibitors: structure-based design, synthesis, and biological evaluation. | J Med Chem 39: 3278-90 (1996) | University of Illinois at Chicago | 2D 3D TSV |
8765510 | 100 | 3-(2-Benzofuranyl)quinuclidin-2-ene derivatives: novel muscarinic antagonists. | J Med Chem 39: 3269-77 (1996) | Uppsala University | 2D 3D TSV |
8765507 | 20 | Synthesis and structure-activity relationships of 1,2,3,4-tetrahydroquinoline-2,3,4-trione 3-oximes: novel and highly potent antagonists for NMDA receptor glycine site. | J Med Chem 39: 3248-55 (1996) | CoCensys Inc | 2D 3D TSV |
8765505 | 26 | Structural modifications of thalidomide produce analogs with enhanced tumor necrosis factor inhibitory activity. | J Med Chem 39: 3238-40 (1996) | Celgene Corporation | 2D 3D TSV |
8765504 | 34 | (S)-(-)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine maleate (SIB-1508Y): a novel anti-parkinsonian agent with selectivity for neuronal nicotinic acetylcholine receptors. | J Med Chem 39: 3235-7 (1996) | SIBIA Neurosciences Inc | 2D 3D TSV |
8765503 | 39 | Identification of the first retinoid X, receptor homodimer antagonist. | J Med Chem 39: 3229-34 (1996) | Ligand Pharmaceuticals Inc | 2D 3D TSV |
8759643 | 17 | Aza-peptide analogs as potent human immunodeficiency virus type-1 protease inhibitors with oral bioavailability. | J Med Chem 39: 3203-16 (1996) | Ciba-Geigy Ltd | 2D 3D TSV |
8759642 | 53 | 1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3. | J Med Chem 39: 3195-202 (1996) | Universit£ di Bari | 2D 3D TSV |
8759641 | 48 | A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid. | J Med Chem 39: 3188-94 (1996) | Royal Danish School of Pharmacy | 2D 3D TSV |
8759640 | 61 | Aryl 1-but-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines as potential antipsychotic agents: synthesis and structure-activity relationships. | J Med Chem 39: 3179-87 (1996) | Warner-Lambert Company | 2D 3D TSV |
8759639 | 33 | Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance P. | J Med Chem 39: 3174-8 (1996) | Hebrew University of Jerusalem | 2D 3D TSV |
8759638 | 6 | Synthesis and characterization of pseudopeptide bradykinin B2 receptor antagonists containing the 1,3,8-triazaspiro[4.5]decan-4-one ring system. | J Med Chem 39: 3169-73 (1996) | Scios Nova Inc | 2D 3D TSV |
8759636 | 1 | Structure-activity relationships of (E)-3-(1,4-benzoquinonyl)-2-[(3-pyridyl)-alkyl]-2-propenoic acid derivatives that inhibit both 5-lipoxygenase and thromboxane A2 synthetase. | J Med Chem 39: 3148-57 (1996) | Eisai Company, Ltd | 2D 3D TSV |
8759635 | 16 | Orally active fibrinogen receptor antagonists. 2. Amidoximes as prodrugs of amidines. | J Med Chem 39: 3139-47 (1996) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
8759634 | 54 | Antipsoriatic anthrones with modulated redox properties. 3. 10-thio-substituted 1,8-dihydroxy-9(10H)-anthracenones as inhibitors of keratinocyte growth, 5-lipoxygenase, and the formation of 12(S)-HETE in mouse epidermis. | J Med Chem 39: 3132-8 (1996) | Universität Regensburg | 2D 3D TSV |
8759633 | 20 | Synthesis and evaluation of phorboid 20-homovanillates: discovery of a class of ligands binding to the vanilloid (capsaicin) receptor with different degrees of cooperativity. | J Med Chem 39: 3123-31 (1996) | Institute | 2D 3D TSV |
8759629 | 11 | Synthesis of 2-amido-2,3-dihydro-1H-phenalene derivatives as new conformationally restricted ligands for melatonin receptors. | J Med Chem 39: 3089-95 (1996) | CNRS-BIOCIS | 2D 3D TSV |
8759625 | 1 | Mechanism-based inhibition of L-pipecolate oxidase by 4,5-dehydro-L-pipecolic acid. | J Med Chem 39: 3046-8 (1996) | Oregon State University | 2D 3D TSV |
8759624 | 1 | Potent inhibition of tumor necrosis factor-alpha production by tetrafluorothalidomide and tetrafluorophthalimides. | J Med Chem 39: 3044-5 (1996) | Institute of Technology | 2D 3D TSV |
8759623 | 31 | Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group. | J Med Chem 39: 3039-43 (1996) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
8759622 | 15 | Identification of a retinoic acid receptor alpha subtype specific agonist. | J Med Chem 39: 3035-8 (1996) | Allergan Inc | 2D 3D TSV |
8759171 | 4 | Lycaconitine revisited: partial synthesis and neuronal nicotinic acetylcholine receptor affinities. | J Nat Prod 59: 707-9 (1996) | Ohio Northern University | 2D 3D TSV |
8730754 | 7 | Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist. | Br J Pharmacol 117: 1558-64 (1996) | University of Occupational and Environmental Health | 2D 3D TSV |
8730737 | 23 | Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety. | Br J Pharmacol 117: 1443-8 (1996) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8723491 | 8 | Anti-influenza virus activities of 4-substituted 2,4-dioxobutanoic acid inhibitors. | Antimicrob Agents Chemother 40: 1304-7 (1996) | Merck Research Laboratories | 2D 3D TSV |
8719416 | 17 | Cloning and characterization of the human GABAA receptor alpha 4 subunit: identification of a unique diazepam-insensitive binding site. | Eur J Pharmacol 291: 319-25 (1995) | CoCensys Inc | 2D 3D TSV |
8709137 | 14 | 3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists. | J Med Chem 39: 3030-4 (1996) | Glaxo Wellcome Research and Development | 2D 3D TSV |
8709135 | 20 | Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology. | J Med Chem 39: 3014-8 (1996) | Warner-Lambert Company | 2D 3D TSV |
8709134 | 26 | Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine. | J Med Chem 39: 3001-13 (1996) | Ohio State University | 2D 3D TSV |
8709132 | 92 | Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors. | J Med Chem 39: 2980-9 (1996) | National Institute of Diabetes | 2D 3D TSV |
8709131 | 42 | Synthesis and activity of a novel series of 3-biarylquinuclidine squalene synthase inhibitors. | J Med Chem 39: 2971-9 (1996) | Zeneca Pharmaceuticals | 2D 3D TSV |
8709129 | 18 | Dihydrobenzofuran analogues of hallucinogens. 3. Models of 4-substituted (2,5-dimethoxyphenyl)alkylamine derivatives with rigidified methoxy groups. | J Med Chem 39: 2953-61 (1996) | Purdue University | 2D 3D TSV |
8709128 | 11 | Similarities and differences in the structure-activity relationships of capsaicin and resiniferatoxin analogues. | J Med Chem 39: 2939-52 (1996) | Institute for Medical Research | 2D 3D TSV |
8709127 | 29 | Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers. | J Med Chem 39: 2922-38 (1996) | Universit£ di Siena | 2D 3D TSV |
8709125 | 11 | N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists. | J Med Chem 39: 2907-14 (1996) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
8709120 | 17 | (S)-(+)-2-(3'-carboxybicyclo[1.1.1]pentyl)-glycine, a structurally new group I metabotropic glutamate receptor antagonist. | J Med Chem 39: 2874-6 (1996) | Università di Perugia | 2D 3D TSV |
8709117 | 7 | New steroidal diazo ketones as potential photoaffinity labeling reagents for the mineralocorticoid receptor: synthesis and biological activities. | J Med Chem 39: 2860-4 (1996) | Université P. et M. Curie | 2D 3D TSV |
8709110 | 27 | Bis tertiary amide inhibitors of the HIV-1 protease generated via protein structure-based iterative design. | J Med Chem 39: 2795-811 (1996) | Agouron Pharmaceuticals Inc | 2D 3D TSV |
8709109 | 18 | Structure-based design and synthesis of substituted 2-butanols as nonpeptidic inhibitors of HIV protease: secondary amide series. | J Med Chem 39: 2781-94 (1996) | Agouron Pharmaceuticals Inc | 2D 3D TSV |
8709108 | 28 | Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus. | J Med Chem 39: 2773-80 (1996) | Eli Lilly and Company | 2D 3D TSV |
8709107 | 99 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. | J Med Chem 39: 2764-72 (1996) | Yamanouchi Pharmaceutical Company Limited | 2D 3D TSV |
8709106 | 89 | Synthesis, ligand binding, and quantitative structure-activity relationship study of 3 beta-(4'-substituted phenyl)-2 beta-heterocyclic tropanes: evidence for an electrostatic interaction at the 2 beta-position. | J Med Chem 39: 2753-63 (1996) | Research Triangle Institute | 2D 3D TSV |
8709105 | 134 | Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. | J Med Chem 39: 2745-52 (1996) | Food and Drug Administration | 2D 3D TSV |
8709104 | 10 | Novel cyclic analogs of angiotensin II with cyclization between positions 5 and 7: conformational and biological implications. | J Med Chem 39: 2738-44 (1996) | Washington University | 2D 3D TSV |
8709099 | 20 | Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans. | J Med Chem 39: 2696-704 (1996) | Tan£be Seiyaku Company, Ltd. | 2D 3D TSV |
8709096 | 26 | Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity. | J Med Chem 39: 2672-80 (1996) | Universitá di Siena | 2D 3D TSV |
8709095 | 87 | (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. | J Med Chem 39: 2664-71 (1996) | Eli Lilly and Company | 2D 3D TSV |
8709094 | 41 | Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells. | J Med Chem 39: 2659-63 (1996) | Ligand Pharmaceuticals Inc | 2D 3D TSV |
8709093 | 21 | 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents. | J Med Chem 39: 2655-8 (1996) | Glaxo Wellcome Research and Development | 2D 3D TSV |
8709092 | 21 | Modulators of leukotriene biosynthesis and receptor activation. | J Med Chem 39: 2629-54 (1996) | Abbott Laboratories | 2D 3D TSV |
8699190 | 9 | Effect of Polygonum hydropiper sulfated flavonoids on lens aldose reductase and related enzymes. | J Nat Prod 59: 443-5 (1996) | Fukuyama University | 2D 3D TSV |
8699182 | 1 | Comparative study of the vasodilatory effects of three quinazoline alkaloids isolated from Evodia rutaecarpa. | J Nat Prod 59: 374-8 (1996) | National Research Instituter of Chinese Medicine | 2D 3D TSV |
8691489 | 12 | Synthesis and ligand binding of eta(6)-(2beta-carbomethoxy-3beta-phenyltropane) transition metal complexes. | J Med Chem 39: 1560-3 (1996) | University of New Orleans | 2D 3D TSV |
8691487 | 21 | Inhibition of human glutathione reductase by 10-arylisoalloxazines: crystalline, kinetic, and electrochemical studies. | J Med Chem 39: 1549-54 (1996) | Institut für Biochemie II der Universität | 2D 3D TSV |
8691482 | 25 | A structure-activity relationship study of novel phenylacetamides which are sodium channel blockers. | J Med Chem 39: 1514-20 (1996) | Warner-Lambert Company | 2D 3D TSV |
8691479 | 24 | trans-2-Aryl-N,N-dipropylcyclopropylamines: synthesis and interactions with 5-HT(1A) receptors. | J Med Chem 39: 1485-93 (1996) | Uppsala University | 2D 3D TSV |
8691478 | 25 | Bradykinin receptor antagonists containing N-substituted amino acids: in vitro and in vivo B(2) and B(1) receptor antagonist activity. | J Med Chem 39: 1472-84 (1996) | Cortech, Inc. | 2D 3D TSV |
8691477 | 28 | N6,C8-distributed adenosine derivatives as partial agonists for adenosine A1 receptors. | J Med Chem 39: 1463-71 (1996) | Leiden/Amsterdam Center for Drug Research | 2D 3D TSV |
8691474 | 111 | 2,4-diamino-5-deaza-6-substituted pyrido[2,3-d]pyrimidine antifolates as potent and selective nonclassical inhibitors of dihydrofolate reductases. | J Med Chem 39: 1438-46 (1996) | Duquesne University | 2D 3D TSV |
8691472 | 49 | Acyl-CoA:Cholesterol O-acyltransferase (ACAT) inhibitors. 2. 2-(1,3-Dioxan-2-yl)-4,5-diphenyl-1H-imidazoles as potent inhibitors of ACAT. | J Med Chem 39: 1423-32 (1996) | Rhône-Poulenc Rorer | 2D 3D TSV |
8691471 | 16 | The squalestatins: inhibitors of squalene synthase. Enzyme inhibitory activities and in vivo evaluation of C3-modified analogues. | J Med Chem 39: 1413-22 (1996) | Glaxo Wellcome Research and Development | 2D 3D TSV |
8691465 | 4 | Ligand interactions with E-selectin. Identification of a new binding site for recognition of N-acyl aromatic glucosamine substituents of sialyl Lewis X. | J Med Chem 39: 1357-60 (1996) | Cytel Corporation | 2D 3D TSV |
8691464 | 9 | Geranylgeranyl diphosphate-based inhibitors of post-translational geranylgeranylation of cellular proteins. | J Med Chem 39: 1352-6 (1996) | Università di Pisa | 2D 3D TSV |
8691463 | 3 | Active site directed inhibition of estrone sulfatase by nonsteroidal coumarin sulfamates. | J Med Chem 39: 1349-51 (1996) | University of Bath | 2D 3D TSV |
8691462 | 14 | 2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase. | J Med Chem 39: 1345-8 (1996) | Merck Research Laboratories | 2D 3D TSV |
8691459 | 24 | Alkyl and alkoxyethyl antineoplastic phospholipids. | J Med Chem 39: 2609-14 (1996) | National Hellenic Research Foundation | 2D 3D TSV |
8691458 | 60 | Design of orally active dual inhibitors of neutral endopeptidase and angiotensin-converting enzyme with long duration of action. | J Med Chem 39: 2594-608 (1996) | University of Paris | 2D 3D TSV |
8691457 | 12 | Synthesis and biological activity of 3- and 5-amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. | J Med Chem 39: 2586-93 (1996) | Yale University | 2D 3D TSV |
8691456 | 7 | Esters and amides of 6-(chloromethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid as inhibitors of alpha-chymotrypsin: significance of the"aromatic" nature of the novel ester-type coumarin for strong inhibitory activity. | J Med Chem 39: 2579-85 (1996) | Université de Liège | 2D 3D TSV |
8691453 | 42 | Synthesis of 3 beta-aryl-8-azabicyclo[3.2.1]octanes with high binding affinities and selectivities for the serotonin transporter site. | J Med Chem 39: 2554-8 (1996) | State University of New York | 2D 3D TSV |
8691452 | 1 | Molecular modeling and site-directed mutagenesis studies of a phorbol ester-binding site in protein kinase C. | J Med Chem 39: 2541-53 (1996) | National Cancer Institute-Bethesda | 2D 3D TSV |
8691451 | 7 | Synthesis and biological evaluation of N alpha-(4-amino-4-deoxy-10-methylpteroyl)-DL-4,4-difluoroornithine. | J Med Chem 39: 2536-40 (1996) | University of Michigan | 2D 3D TSV |
8691450 | 49 | Synthesis and biological evaluation of new imidazole, pyrimidine, and purine derivatives and analogs as inhibitors of xanthine oxidase. | J Med Chem 39: 2529-35 (1996) | Università di Modena | 2D 3D TSV |
8691445 | 70 | Chiral pyrrolo[2,3-d]pyrimidine and pyrimido[4,5-b]indole derivatives: structure-activity relationships of potent, highly stereoselective A1-adenosine receptor antagonists. | J Med Chem 39: 2482-91 (1996) | Julius-Maximilians-Universität Würzburg | 2D 3D TSV |
8691444 | 105 | Antiretroviral agents as inhibitors of both human immunodeficiency virus type 1 integrase and protease. | J Med Chem 39: 2472-81 (1996) | National Cancer Institute-Bethesda | 2D 3D TSV |
8691442 | 52 | Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency. | J Med Chem 39: 2456-60 (1996) | University of Arizona | 2D 3D TSV |
8691441 | 19 | Topographical amino acid substitution in position 10 of glucagon leads to antagonists/partial agonists with greater binding differences. | J Med Chem 39: 2449-55 (1996) | University of Arizona | 2D 3D TSV |
8691440 | 22 | Synthesis of potent cyclic hexapeptide NK-1 antagonists. Use of a minilibrary in transforming a peptidal somatostatin receptor ligand into an NK-1 receptor ligand via a polyvalent peptidomimetic. | J Med Chem 39: 2441-8 (1996) | University of Pennsylvania | 2D 3D TSV |
8691438 | 48 | (S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. | J Med Chem 39: 2435-7 (1996) | Pharmacia & Upjohn | 2D 3D TSV |
8691435 | 33 | Retinoic acid receptor beta,gamma-selective ligands: synthesis and biological activity of 6-substituted 2-naphthoic acid retinoids. | J Med Chem 39: 2411-21 (1996) | Pharmaceutical Research Institute | 2D 3D TSV |
8691434 | 25 | Structure-based design of novel HIV protease inhibitors: sulfonamide-containing 4-hydroxycoumarins and 4-hydroxy-2-pyrones as potent non-peptidic inhibitors. | J Med Chem 39: 2400-10 (1996) | Upjohn | 2D 3D TSV |
8691433 | 2 | New neplanocin analogues. 6. Synthesis and potent antiviral activity of 6'-homoneplanocin A1. | J Med Chem 39: 2392-9 (1996) | Hokkaido University | 2D 3D TSV |
8691432 | 79 | New prolyl endopeptidase inhibitors: in vitro and in vivo activities of azabicyclo[2.2.2]octane, azabicyclo[2.2.1]heptane, and perhydroindole derivatives. | J Med Chem 39: 2379-91 (1996) | Institut de Recherche Servier | 2D 3D TSV |
8691430 | 42 | Inhibitors of acyl-CoA:cholesterol O-acyltransferase. synthesis and pharmacological activity of (+/-)-2-dodecyl-alpha-phenyl-N-(2,4,6-trimethoxyphenyl)-2H-tetrazole-5- acetamide and structurally related tetrazole amide derivatives. | J Med Chem 39: 2354-66 (1996) | Warner-Lambert Company | 2D 3D TSV |
8691429 | 4 | Aristeromycin-5'-carboxaldehyde: a potent inhibitor of S-adenosyl-L-homocysteine hydrolase. | J Med Chem 39: 2347-53 (1996) | University of Kansas | 2D 3D TSV |
8691428 | 1 | Ryanodine action at calcium release channels. 2. relation to substituents of the cyclohexane ring. | J Med Chem 39: 2339-46 (1996) | University of California | 2D 3D TSV |
8691427 | 3 | Ryanodine action at calcium release channels. 1. importance of hydroxyl substituents. | J Med Chem 39: 2331-8 (1996) | University of California | 2D 3D TSV |
8691426 | 114 | Synthesis and structure-activity relationships of 2-substituted D-tryptophan-containing peptidic endothelin receptor antagonists: importance of the C-2 substituent of the D-tryptophan residue for endothelin A and B receptor subtype selectivity. | J Med Chem 39: 2313-30 (1996) | Tsukuba Research Institute | 2D 3D TSV |
8691425 | 23 | Structural and stereoelectronic requirements for the inhibition of mammalian 2,3-oxidosqualene cyclase by substituted isoquinoline derivatives. | J Med Chem 39: 2302-12 (1996) | Laboratoires Fournier SCA | 2D 3D TSV |
8691424 | 61 | Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. | J Med Chem 39: 2293-301 (1996) | National Institute of Diabetes | 2D 3D TSV |
8691423 | 89 | 4-(Phenylamino)pyrrolopyrimidines: potent and selective, ATP site directed inhibitors of the EGF-receptor protein tyrosine kinase. | J Med Chem 39: 2285-92 (1996) | CIBA Pharmaceuticals | 2D 3D TSV |
8691422 | 25 | 2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor. | J Med Chem 39: 2281-4 (1996) | SmithKline Beecham S.p.A. | 2D 3D TSV |
8676355 | 90 | Structure-activity relationships of a series of substituted benzamides: potent D2/5-HT2 antagonists and 5-HT1a agonists as neuroleptic agents. | J Med Chem 39: 1172-88 (1996) | Glaxo Wellcome Inc. | 2D 3D TSV |
8676354 | 42 | Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists. | J Med Chem 39: 1164-71 (1996) | Università degli Studi di Ferrara | 2D 3D TSV |
8676353 | 140 | Novel carbamates as potent histamine H3 receptor antagonists with high in vitro and oral in vivo activity. | J Med Chem 39: 1157-63 (1996) | Freie Universität Berlin | 2D 3D TSV |
8676350 | 39 | Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2. | J Med Chem 39: 1136-41 (1996) | University of Arizona | 2D 3D TSV |
8676348 | 10 | 8-[4-[2-(1,2,3,4-Tetrahydroisoquinolinyl]butyl-8-azaspiro[4.5]decane-7,9-dione: a new 5-HT1A receptor ligand with the same activity profile as buspirone. | J Med Chem 39: 1125-9 (1996) | Polish Academy of Sciences | 2D 3D TSV |
8676347 | 39 | Nonpeptidic inhibitors of human neutrophil elastase. 7. Design, synthesis, and in vitro activity of a series of pyridopyrimidine trifluoromethyl ketones. | J Med Chem 39: 1112-24 (1996) | Zeneca Pharmaceuticals | 2D 3D TSV |
8676339 | 143 | 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722. | J Med Chem 39: 1039-48 (1996) | Abbott Laboratories | 2D 3D TSV |
8676338 | 16 | Time-dependent inactivation of aromatase by 6-alkylandrosta-1,4-diene-3,17-diones. Effects of length and configuration of 6-alkyl group. | J Med Chem 39: 1033-8 (1996) | Tohoku College of Pharmacy | 2D 3D TSV |
8676336 | 2 | 4'-O-[2-(2-fluoromalonyl)]-L-tyrosine: a phosphotyrosyl mimic for the preparation of signal transduction inhibitory peptides. | J Med Chem 39: 1021-7 (1996) | National Cancer Institute-Bethesda | 2D 3D TSV |
8676335 | 2 | Carbohydrates in an acidic multivalent assembly: nanomolar P-selectin inhibitors. | J Med Chem 39: 1018-20 (1996) | Lawrence Berkeley National Laboratories | 2D 3D TSV |
8676334 | 9 | Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents. | J Med Chem 39: 1016-7 (1996) | University of North Carolina at Chapel Hill | 2D 3D TSV |
8676333 | 46 | N-terminus urea-substituted chemotactic peptides: new potent agonists and antagonists toward the neutrophil fMLF receptor. | J Med Chem 39: 1013-5 (1996) | Johnson Matthey Biomedical Research | 2D 3D TSV |
8676127 | 40 | Effects of Various Isoquinoline Alkaloids on In Vitro 3H-Dopamine Uptake by Rat Striatal Synaptosomes | J Nat Prod 58: 1475-1484 (1995) | TBA | 2D 3D TSV |
8670053 | 3 | ATP-dependent glutathione disulphide transport mediated by the MRP gene-encoded conjugate export pump. | Biochem J 314: 433-7 (1996) | Deutsches Krebsforschungszentrum | 2D 3D TSV |
8667369 | 121 | Synthesis and pharmacological characterization of all sixteen stereoisomers of 2-(2'-carboxy-3'-phenylcyclopropyl)glycine. Focus on (2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine, a novel and selective group II metabotropic glutamate receptors antagonist. | J Med Chem 39: 2259-69 (1996) | Università di Perugia | 2D 3D TSV |
8667368 | 42 | Synthesis, absolute configuration, and biological profile of the enantiomers of trans-[2-(2,6-dimethoxyphenoxy)ethyl] [(3-p-tolyl-2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amine (mephendioxan), a potent competitive alpha 1A-adrenoreceptor antagonist. | J Med Chem 39: 2253-8 (1996) | University of Camerino | 2D 3D TSV |
8667367 | 28 | Synthesis and structure-activity relationships of 6-substituted androst-4-ene analogs as aromatase inhibitors. | J Med Chem 39: 2245-52 (1996) | Tohoku College of Pharmacy | 2D 3D TSV |
8667363 | 1 | Diphenylpropionic acids as new AT1 selective angiotensin II antagonists. | J Med Chem 39: 2197-206 (1996) | J. Uriach & Cia SA | 2D 3D TSV |
8667361 | 23 | Ureido-based peptidomimetic inhibitor of herpes simplex virus ribonucleotide reductase: an investigation of inhibitor bioactive conformation. | J Med Chem 39: 2178-87 (1996) | Bio-Méga/Boehringer Ingelheim Research Inc. | 2D 3D TSV |
8667360 | 46 | Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins. | J Med Chem 39: 2170-7 (1996) | Hebrew University of Jerusalem | 2D 3D TSV |
8667359 | 36 | Preparation and structure-activity relationship of novel P1/P1'-substituted cyclic urea-based human immunodeficiency virus type-1 protease inhibitors. | J Med Chem 39: 2156-69 (1996) | DuPont Pharmaceuticals Company | 2D 3D TSV |
8667357 | 33 | Comparative molecular moment analysis (CoMMA): 3D-QSAR without molecular superposition. | J Med Chem 39: 2129-40 (1996) | IBM Thomas J. Watson Research Center | 2D 3D TSV |
8667356 | 50 | Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists. | J Med Chem 39: 2123-8 (1996) | BASF AG | 2D 3D TSV |
8667355 | 2 | Discovery of an orally active non-peptide fibrinogen receptor antagonist. | J Med Chem 39: 2118-22 (1996) | Hoechst AG | 2D 3D TSV |
8667026 | 14 | The C-terminal domain of the mGluR1 metabotropic glutamate receptor affects sensitivity to agonists. | J Neurochem 67: 58-63 (1996) | CNS Research | 2D 3D TSV |
8666985 | 12 | Similarity between rat brain nicotinic alpha-bungarotoxin receptors and stably expressed alpha-bungarotoxin binding sites. | J Neurochem 67: 145-54 (1996) | McGill University | 2D 3D TSV |
8663568 | 17 | Cloning and expression of a novel neuropeptide Y receptor. | J Biol Chem 271: 16435-8 (1996) | Merck Research Laboratories | 2D 3D TSV |
8648612 | 30 | Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells. | J Med Chem 39: 1729-35 (1996) | University of Minnesota | 2D 3D TSV |
8648610 | 35 | Inhibitors of acyl CoA:cholesterol acyltransferase. | J Med Chem 39: 1704-19 (1996) | Schering-Plough Research Institute | 2D 3D TSV |
8648609 | 15 | Design, synthesis, and biochemical evaluation of N-substituted maleimides as inhibitors of prostaglandin endoperoxide synthases. | J Med Chem 39: 1692-703 (1996) | Vanderbilt University School of Medicine | 2D 3D TSV |
8648606 | 72 | Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists. | J Med Chem 39: 1664-75 (1996) | Cambridge University Forvie Site | 2D 3D TSV |
8648604 | 15 | All-atom models for the non-nucleoside binding site of HIV-1 reverse transcriptase complexed with inhibitors: a 3D QSAR approach. | J Med Chem 39: 1645-50 (1996) | National Cancer Institute-Frederick | 2D 3D TSV |
8648603 | 101 | Synthesis and cyclic GMP phosphodiesterase inhibitory activity of a series of 6-phenylpyrazolo[3,4-d]pyrimidones. | J Med Chem 39: 1635-44 (1996) | Laboratories Glaxo Wellcome Centre de Recherches | 2D 3D TSV |
8648598 | 3 | Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent non-nucleoside inhibitors. | J Med Chem 39: 1589-600 (1996) | Oxford University | 2D 3D TSV |
8648595 | 7 | Conformationally restricted TRH analogs: a probe for the pyroglutamate region. | J Med Chem 39: 1571-4 (1996) | Washington University | 2D 3D TSV |
8643460 | 10 | Cloning and functional expression of cDNAs encoding human and rat pancreatic polypeptide receptors. | Proc Natl Acad Sci U S A 93: 4661-5 (1996) | Amgen Inc | 2D 3D TSV |
8642569 | 23 | Design and synthesis of new linear and cyclic bradykinin antagonists. | J Med Chem 39: 2095-101 (1996) | Institute de Recherches Servier | 2D 3D TSV |
8642568 | 28 | Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides. | J Med Chem 39: 2087-94 (1996) | Boehringer Ingelheim Pharmaceuticals Inc | 2D 3D TSV |
8642567 | 64 | Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity. | J Med Chem 39: 2081-6 (1996) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8642566 | 277 | Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines. | J Med Chem 39: 2068-80 (1996) | Universit£ de Caen | 2D 3D TSV |
8642565 | 36 | Inhibitors of human immunodeficiency virus type 1 protease containing 2-aminobenzyl-substituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, activity, and oral bioavailability. | J Med Chem 39: 2060-7 (1996) | Sandoz Research Institute | 2D 3D TSV |
8642564 | 12 | Studies on selectin blockers. 2. Novel selectin blocker as potential therapeutics for inflammatory disorders. | J Med Chem 39: 2055-9 (1996) | New Drug Research Laboratory | 2D 3D TSV |
8642563 | 18 | Discovery of novel, non-peptide HIV-1 protease inhibitors by pharmacophore searching. | J Med Chem 39: 2047-54 (1996) | National Institutes of Health | 2D 3D TSV |
8642558 | 30 | Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity. | J Med Chem 39: 1991-2007 (1996) | Bristol-Myers Squibb Co. | 2D 3D TSV |
8642556 | 1 | Antitumor agents. 166. Synthesis and biological evaluation of 5,6,7,8-substituted-2-phenylthiochromen-4-ones. | J Med Chem 39: 1975-80 (1996) | University of North Carolina | 2D 3D TSV |
8642555 | 11 | (Aminoalkyl)indole isothiocyanates as potential electrophilic affinity ligands for the brain cannabinoid receptor. | J Med Chem 39: 1967-74 (1996) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8642554 | 42 | Asymmetric syntheses, opioid receptor affinities, and antinociceptive effects of 8-amino-5,9-methanobenzocyclooctenes, a new class of structural analogues of the morphine alkaloids. | J Med Chem 39: 1956-66 (1996) | Institute | 2D 3D TSV |
8642552 | 20 | Design and synthesis of 2-naphthoate esters as selective dopamine D4 antagonists. | J Med Chem 39: 1946-8 (1996) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8642551 | 27 | 5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors. | J Med Chem 39: 1943-5 (1996) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
8642550 | 30 | 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. | J Med Chem 39: 1941-2 (1996) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
8640791 | 1 | Transport of glutathione, glucuronate, and sulfate conjugates by the MRP gene-encoded conjugate export pump. | Cancer Res 56: 988-94 (1996) | Deutsches Krebsforschungszentrum | 2D 3D TSV |
8632757 | 19 | Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. | Mol Pharmacol 49: 253-9 (1996) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
8632441 | 24 | Studies on selectin blocker. 1. Structure-activity relationships of sialyl Lewis X analogs. | J Med Chem 39: 1339-43 (1996) | Institute of Cancer Research | 2D 3D TSV |
8632440 | 2 | Novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonists: synthesis and structure-activity relationships of 6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-pyrido[2,3-b]pyrazinedione and related compounds. | J Med Chem 39: 1331-8 (1996) | Yamanouchi Pharmaceutical Company Limited | 2D 3D TSV |
8632437 | 8 | Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. | J Med Chem 39: 1303-13 (1996) | MediChem Research, Inc. | 2D 3D TSV |
8632434 | 198 | Lipophilic antifolates as agents against opportunistic infections. 1. Agents superior to trimetrexate and piritrexim against Toxoplasma gondii and Pneumocystis carinii in in vitro evaluations. | J Med Chem 39: 1271-80 (1996) | Southern Research Institute | 2D 3D TSV |
8632433 | 36 | Potent inhibitors of acyl-CoA:cholesterol acyltransferase. 2. Structure-activity relationships of novel N-(2,2-dimethyl-2,3-dihydrobenzofuran-7-yl)amides. | J Med Chem 39: 1262-70 (1996) | Institute for Bio-Medical Research | 2D 3D TSV |
8632431 | 167 | Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate. | J Med Chem 39: 1243-52 (1996) | Warner-Lambert Company | 2D 3D TSV |
8632428 | 63 | [125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor. | J Med Chem 39: 1220-6 (1996) | Freie Universität Berlin | 2D 3D TSV |
8632427 | 80 | Optimal recognition of neutral endopeptidase and angiotensin-converting enzyme active sites by mercaptoacyldipeptides as a means to design potent dual inhibitors. | J Med Chem 39: 1210-9 (1996) | University of Paris | 2D 3D TSV |
8632426 | 62 | Synthesis and pharmacology of potential cocaine antagonists. 2. Structure-activity relationship studies of aromatic ring-substituted methylphenidate analogs. | J Med Chem 39: 1201-9 (1996) | Georgia Institute of Technology | 2D 3D TSV |
8632424 | 16 | Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. | J Med Chem 39: 1193-5 (1996) | Allergan Inc | 2D 3D TSV |
8632423 | 16 | Homologs of idoxifene: variation of estrogen receptor binding and calmodulin antagonism with chain length. | J Med Chem 39: 999-1004 (1996) | Institute of Cancer Research | 2D 3D TSV |
8632421 | 32 | Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption. | J Med Chem 39: 982-91 (1996) | Abbott Laboratories | 2D 3D TSV |
8632420 | 112 | Azole endothelin antagonists. 2. Structure-activity studies. | J Med Chem 39: 968-81 (1996) | Abbott Laboratories | 2D 3D TSV |
8632419 | 50 | Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile. | J Med Chem 39: 957-67 (1996) | Abbott Laboratories | 2D 3D TSV |
8632418 | 21 | Guanine, pyrazolo[3,4-d]pyrimidine, and triazolo[4,5-d]pyrimidine (8-azaguanine) phosphonate acyclic derivatives as inhibitors of purine nucleoside phosphorylase. | J Med Chem 39: 949-56 (1996) | Burroughs Wellcome Co. | 2D 3D TSV |
8632415 | 17 | Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor. | J Med Chem 39: 918-28 (1996) | University of Auckland | 2D 3D TSV |
8632413 | 38 | High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size. | J Med Chem 39: 892-903 (1996) | Wellcome Research Laboratories | 2D 3D TSV |
8632410 | 33 | Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors. | J Med Chem 39: 860-72 (1996) | Universitá di Siena | 2D 3D TSV |
8632409 | 15 | Comparative molecular field analysis-based prediction of drug affinities at recombinant D1A dopamine receptors. | J Med Chem 39: 850-9 (1996) | VA Medical Center | 2D 3D TSV |
8632408 | 24 | Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas. | J Med Chem 39: 842-9 (1996) | Neuroscience Research Centre | 2D 3D TSV |
8632407 | 43 | Tetrahydronaphthalenes: influence of heterocyclic substituents on inhibition of steroid enzymes P450 arom and P450 17. | J Med Chem 39: 834-41 (1996) | Universität de Saarlandes | 2D 3D TSV |
8632404 | 3 | (2S,4S)-2-amino-4-(4,4-diphenylbut-1-yl)- pentane-1,5-dioic acid: a potent and selective antagonist for metabotropic glutamate receptors negatively linked to adenylate cyclase. | J Med Chem 39: 814-6 (1996) | Centre de Neurochimie du CNRS | 2D 3D TSV |
8632403 | 14 | Bis(31/31') ([CYS(31), Trp(32), Nva(34)] NPY-(31-36)): a specific NPY Y-1 receptor antagonist. | J Med Chem 39: 811-3 (1996) | University of Cincinnati Medical Center | 2D 3D TSV |
8632342 | 110 | Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences. | J Pharmacol Exp Ther 276: 720-7 (1996) | Eli Lilly and Company | 2D 3D TSV |
8627617 | 47 | Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors. | J Med Chem 39: 1928-34 (1996) | University of Wisconsin-Milwaukee | 2D 3D TSV |
8627616 | 12 | Highly selective aldose reductase inhibitors. 1. 3-(Arylalkyl)-2,4,5-trioxoimidazolidine-1-acetic acids. | J Med Chem 39: 1924-7 (1996) | Nippon Zoki Pharmaceutical Company Ltd | 2D 3D TSV |
8627615 | 16 | 2-(Hydroxyalkyl)estradiols: synthesis and biological evaluation. | J Med Chem 39: 1917-23 (1996) | Ohio State University | 2D 3D TSV |
8627611 | 17 | Structure-based design of novel, urea-containing FKBP12 inhibitors. | J Med Chem 39: 1872-84 (1996) | Agouron Pharmaceuticals Inc | 2D 3D TSV |
8627609 | 51 | Selective inhibitors of monoamine oxidase. 3. Structure-activity relationship of tricyclics bearing imidazoline, oxadiazole, or tetrazole groups. | J Med Chem 39: 1857-63 (1996) | Wellcome Research Laboratories | 2D 3D TSV |
8627608 | 100 | Novel terphenyls as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents. | J Med Chem 39: 1846-56 (1996) | Searle Research and Development | 2D 3D TSV |
8627607 | 147 | Nonclassical 2,4-diamino-8-deazafolate analogues as inhibitors of dihydrofolate reductases from rat liver, Pneumocystis carinii, and Toxoplasma gondii. | J Med Chem 39: 1836-45 (1996) | Duquesne University | 2D 3D TSV |
8627606 | 47 | Tyrosine Kinase Inhibitors. 10. Isomeric 4-[(3-Bromophenyl)amino]pyrido[d]- pyrimidines Are Potent ATP Binding Site Inhibitors of the Tyrosine Kinase Function of the Epidermal Growth Factor Receptor | J Med Chem 39: 1823-35 (1996) | University of Auckland | 2D 3D TSV |
8627605 | 10 | Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide"address" recognition at kappa opioid receptors. | J Med Chem 39: 1816-22 (1996) | University of Minnesota | 2D 3D TSV |
8627604 | 38 | Non-peptide cholecystokinin-B/gastrin receptor antagonists based on bicyclic, heteroaromatic skeletons. | J Med Chem 39: 1806-15 (1996) | James Black Foundation | 2D 3D TSV |
8627603 | 58 | Mapping the melatonin receptor. 4. Comparison of the binding affinities of a series of substituted phenylalkyl amides. | J Med Chem 39: 1797-805 (1996) | University College London | 2D 3D TSV |
8627601 | 169 | Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether. | J Med Chem 39: 1778-89 (1996) | Ligand Pharmaceuticals Inc | 2D 3D TSV |
8627599 | 4 | Development of a high specific activity sulfur-35-labeled sulfonamide radioligand that allowed the identification of a new growth hormone secretagogue receptor. | J Med Chem 39: 1767-70 (1996) | Merck Research Laboratories | 2D 3D TSV |
8627597 | 17 | 2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist. | J Med Chem 39: 1760-2 (1996) | Merck Research Laboratories | 2D 3D TSV |
8627580 | 8 | Preclinical characterization of the potential of the putative atypical antipsychotic MDL 100,907 as a potent 5-HT2A antagonist with a favorable CNS safety profile. | J Pharmacol Exp Ther 277: 968-81 (1996) | Hoechst Marion Roussel Inc | 2D 3D TSV |
8627566 | 53 | In vitro and in vivo characterization of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist. | J Pharmacol Exp Ther 277: 840-51 (1996) | Hoechst Marion Roussel Inc | 2D 3D TSV |
8627565 | 2 | Transport characteristics of differently charged cephalosporin antibiotics in oocytes expressing the cloned intestinal peptide transporter PepT1 and in human intestinal Caco-2 cells. | J Pharmacol Exp Ther 277: 831-9 (1996) | University of Giessen | 2D 3D TSV |
8621644 | 9 | ATP-dependent 17 beta-estradiol 17-(beta-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroids. | J Biol Chem 271: 9683-9 (1996) | Queen's University | 2D 3D TSV |
8584042 | 40 | BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex. | Naunyn Schmiedebergs Arch Pharmacol 352: 276-82 (1995) | Boehringer Ingelheim Italia | 2D 3D TSV |
8576924 | 69 | Novel N6-(substituted-phenylcarbamoyl)adenosine-5'-uronamides as potent agonists for A3 adenosine receptors. | J Med Chem 39: 802-6 (1996) | Universit£ di Ferrara | 2D 3D TSV |
8576921 | 63 | Interactions of flavonoids and other phytochemicals with adenosine receptors. | J Med Chem 39: 781-8 (1996) | National Institute of Diabetes | 2D 3D TSV |
8576920 | 34 | Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides. | J Med Chem 39: 773-80 (1996) | University of Ferrara | 2D 3D TSV |
8576919 | 30 | Structure-activity relationships of a new family of steroidal aromatase inhibitors. 1. Synthesis and evaluation of a series of analogs related to 19-[(methylthio)methyl]androstenedione (RU54115). | J Med Chem 39: 757-72 (1996) | Centre de Recherche de Roussel Uclaf | 2D 3D TSV |
8576918 | 38 | Structure-activity relationship studies of novel 4-[2-[bis(4-fluorophenyl)methoxy]ethyl]-1-(3-phenylpropyl)piperidine analogs: synthesis and biological evaluation at the dopamine and serotonin transporter sites. | J Med Chem 39: 749-56 (1996) | Organix Inc | 2D 3D TSV |
8576917 | 79 | 3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists. | J Med Chem 39: 736-48 (1996) | Eli Lilly and Company | 2D 3D TSV |
8576914 | 14 | Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin. | J Med Chem 39: 713-9 (1996) | Glaxo Wellcome Research Institute | 2D 3D TSV |
8576912 | 34 | Quinazoline antifolates thymidylate synthase inhibitors: lipophilic analogues with modification to the C2-methyl substituent. | J Med Chem 39: 695-704 (1996) | Zeneca Pharma | 2D 3D TSV |
8576911 | 4 | Slow-binding inhibition of gamma-aminobutyric acid aminotransferase by hydrazine analogues. | J Med Chem 39: 686-94 (1996) | Northwestern University | 2D 3D TSV |
8576908 | 33 | 2-Iminopiperidine and other 2-iminoazaheterocycles as potent inhibitors of human nitric oxide synthase isoforms. | J Med Chem 39: 669-72 (1996) | G. D. Searle Research and Development | 2D 3D TSV |
8576907 | 13 | The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. | J Med Chem 39: 665-8 (1996) | Glaxo Wellcome Research and Development | 2D 3D TSV |
8576905 | 25 | alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase. | J Med Chem 39: 657-60 (1996) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8576904 | 78 | Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy. | J Med Chem 39: 625-56 (1996) | DuPont Pharmaceuticals Company | 2D 3D TSV |
8568831 | 42 | Potent human immunodeficiency virus type 1 protease inhibitors that utilize noncoded D-amino acids as P2/P3 ligands. | J Med Chem 39: 96-108 (1996) | Eli Lilly and Company | 2D 3D TSV |
8568830 | 2 | (-)-Arctigenin as a lead structure for inhibitors of human immunodeficiency virus type-1 integrase. | J Med Chem 39: 86-95 (1996) | Freie Universität Berlin | 2D 3D TSV |
8568829 | 22 | Quinazoline antifolate thymidylate synthase inhibitors: gamma-linked L-D, D-D, and D-L dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583). | J Med Chem 39: 73-85 (1996) | Institute of Cancer Research | 2D 3D TSV |
8568828 | 2 | Synthesis and biological evaluation of DL-4,4-difluoroglutamic acid and DL-gamma,gamma-difluoromethotrexate. | J Med Chem 39: 66-72 (1996) | University of Michigan | 2D 3D TSV |
8568827 | 6 | Synthesis and biological activity of folic acid and methotrexate analogues containing L-threo-(2S,4S)-4-fluoroglutamic acid and DL-3,3-difluoroglutamic acid. | J Med Chem 39: 56-65 (1996) | University of Michigan | 2D 3D TSV |
8568825 | 13 | Conformationally constrained analogues of diacylglycerol. 12. Ultrapotent protein kinase C ligands based on a chiral 4,4-disubstituted heptono-1,4-lactone template. | J Med Chem 39: 36-45 (1996) | National Cancer Institute-Bethesda | 2D 3D TSV |
8568823 | 36 | Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds. | J Med Chem 39: 323-38 (1996) | Sankyo Company Ltd | 2D 3D TSV |
8568822 | 80 | Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors. | J Med Chem 39: 314-22 (1996) | Virginia Commonwealth University | 2D 3D TSV |
8568820 | 10 | Studies of cardiotonic agents. 8. Synthesis and biological activities of optically active 6-(4-(benzylamino)-7-quinazolinyl)-4,5-dihydro-5-methyl-3(2H)- pyridazinone (KF15232). | J Med Chem 39: 297-303 (1996) | Kyowa Hakka Co., Ltd. | 2D 3D TSV |
8568819 | 6 | Conformationally constrained analogues of diacylglycerol. 11. Ultrapotent protein kinase C ligands based on a chiral 5-disubstituted tetrahydro-2-furanone template. | J Med Chem 39: 29-35 (1996) | National Cancer Institute-Bethesda | 2D 3D TSV |
8568818 | 12 | Conformational analysis of D1 dopamine receptor agonists: pharmacophore assessment and receptor mapping. | J Med Chem 39: 285-96 (1996) | University of North Carolina | 2D 3D TSV |
8568817 | 2 | Theoretical study of inhibition of adenosine deaminase by (8R)-coformycin and (8R)-deoxycoformycin. | J Med Chem 39: 277-84 (1996) | University of California | 2D 3D TSV |
8568816 | 69 | Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure-Activity Relationship for Analogues of 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a Potent Inhibitor of the Epidermal Growth Factor Receptor | J Med Chem 39: 267-76 (1996) | Parke-Davis Pharmaceutical Research | 2D 3D TSV |
8568815 | 70 | Diarylspiro[2.4]heptenes as orally active, highly selective cyclooxygenase-2 inhibitors: synthesis and structure-activity relationships. | J Med Chem 39: 253-66 (1996) | Searle Research and Development | 2D 3D TSV |
8568814 | 23 | Dibenzoxepinone hydroxylamines and hydroxamic acids: dual inhibitors of cyclooxygenase and 5-lipoxygenase with potent topical antiinflammatory activity. | J Med Chem 39: 246-52 (1996) | Hoechst-Roussel Pharmaceuticals Inc | 2D 3D TSV |
8568812 | 36 | Development of highly potent inhibitors of Ras farnesyltransferase possessing cellular and in vivo activity. | J Med Chem 39: 224-36 (1996) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8568811 | 22 | Design and synthesis of non-peptide Ras CAAX mimetics as potent farnesyltransferase inhibitors. | J Med Chem 39: 217-23 (1996) | University of Pittsburgh | 2D 3D TSV |
8568809 | 34 | Substituted xanthines, pteridinediones, and related compounds as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor alpha. | J Med Chem 39: 2-9 (1996) | University of California | 2D 3D TSV |
8568807 | 7 | In vitro and in vivo studies of benzisoquinoline ligands for the brain synaptic vesicle monoamine transporter. | J Med Chem 39: 191-6 (1996) | University of Michigan Medical School | 2D 3D TSV |
8568806 | 9 | Conformationally constrained analogues of diacylglycerol. 10. Ultrapotent protein kinase C ligands based on a racemic 5-disubstituted tetrahydro-2-furanone template. | J Med Chem 39: 19-28 (1996) | National Cancer Institute-Bethesda | 2D 3D TSV |
8568804 | 42 | New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives. | J Med Chem 39: 176-82 (1996) | Universit£ di Bari | 2D 3D TSV |
8568803 | 27 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. | J Med Chem 39: 158-75 (1996) | Upjohn Laboratories | 2D 3D TSV |
8568802 | 42 | Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives. | J Med Chem 39: 149-57 (1996) | Glaxo Wellcome Inc. | 2D 3D TSV |
8568801 | 13 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. | J Med Chem 39: 143-8 (1996) | Pfizer Inc | 2D 3D TSV |
8568800 | 155 | Structure-antigastrin activity relationships of new spiroglumide amido acid derivatives. | J Med Chem 39: 135-42 (1996) | Rotta Research Laboratorium | 2D 3D TSV |
8568799 | 281 | Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models. | J Med Chem 39: 126-34 (1996) | Universit£ de Lausanne | 2D 3D TSV |
8568798 | 29 | Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret. | J Med Chem 39: 120-5 (1996) | Pfizer Inc. | 2D 3D TSV |
8566176 | 79 | Deriving the therapeutic concentrations for clozapine and haloperidol: the apparent dissociation constant of a neuroleptic at the dopamine D2 or D4 receptor varies with the affinity of the competing radioligand. | Eur J Pharmacol 291: 59-66 (1995) | University of Toronto | 2D 3D TSV |
8564266 | 77 | Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed. | Br J Pharmacol 116: 2315-21 (1995) | Vrije Universiteit | 2D 3D TSV |
8564196 | 35 | Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo. | Br J Pharmacol 115: 1387-92 (1995) | Syntex Discovery Research | 2D 3D TSV |
8558536 | 3 | Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alpha-linked acidic dipeptidase. | J Med Chem 39: 619-22 (1996) | Zeneca Pharmaceuticals | 2D 3D TSV |
8558534 | 9 | Aminoacetyl moiety as a potential surrogate for diacylhydrazine group of SC-51089, a potent PGE2 antagonist, and its analogs. | J Med Chem 39: 609-13 (1996) | Searle | 2D 3D TSV |
8558532 | 53 | 2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6-tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors. | J Med Chem 39: 596-604 (1996) | Tanabe Seiyaku Co., Ltd | 2D 3D TSV |
8558530 | 4 | Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease. | J Med Chem 39: 582-7 (1996) | Hoechst-Roussel Pharmaceuticals Inc | 2D 3D TSV |
8558529 | 195 | Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. | J Med Chem 39: 570-81 (1996) | Hoechst-Roussel Pharmaceuticals Inc | 2D 3D TSV |
8558528 | 16 | Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist"trigger". | J Med Chem 39: 562-9 (1996) | Glaxo Wellcome | 2D 3D TSV |
8558526 | 6 | 9-Dihydroxy-2,3,7,11b-tetrahydro-1H-naph[1,2,3-de]isoquinoline: a potent full dopamine D1 agonist containing a rigid-beta-phenyldopamine pharmacophore. | J Med Chem 39: 549-55 (1996) | Purdue University | 2D 3D TSV |
8558525 | 60 | N-substituted analogs of 2 beta-carbomethoxy-3 beta- (4'-iodophenyl)tropane (beta-CIT) with selective affinity to dopamine or serotonin transporters in rat forebrain. | J Med Chem 39: 543-8 (1996) | Research Biochemicals International | 2D 3D TSV |
8558522 | 26 | 2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones. | J Med Chem 39: 522-30 (1996) | Universita di Roma | 2D 3D TSV |
8558518 | 38 | Dual metalloprotease inhibitors. 6. Incorporation of bicyclic and substituted monocyclic azepinones as dipeptide surrogates in angiotensin-converting enzyme/neutral endopeptidase inhibitors. | J Med Chem 39: 494-502 (1996) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8558508 | 55 | Tetrahydrobenzothiophenone derivatives as a novel class of adenosine receptor antagonists. | J Med Chem 39: 398-406 (1996) | National Institute of Diabetes | 2D 3D TSV |
8558507 | 7 | A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease. | J Med Chem 39: 392-7 (1996) | Abbott Laboratories | 2D 3D TSV |
8558505 | 77 | A comparative molecular field analysis study of N-benzylpiperidines as acetylcholinesterase inhibitors. | J Med Chem 39: 380-7 (1996) | University of Missouri St. Louis | 2D 3D TSV |
8558504 | 43 | 2-Carbomethoxy-3-(diarylmethoxy)-1 alpha H, 5 alpha H-tropane analogs: synthesis and inhibition of binding at the dopamine transporter and comparison with piperazines of the GBR series. | J Med Chem 39: 371-9 (1996) | Organix Inc | 2D 3D TSV |
8558503 | 22 | Synthesis and quantitative structure-activity relationship of a novel series of small conductance Ca(2+)-activated K+ channel blockers related to dequalinium. | J Med Chem 39: 359-70 (1996) | University College London | 2D 3D TSV |
8558502 | 17 | Potent, cell active, non-thiol tetrapeptide inhibitors of farnesyltransferase. | J Med Chem 39: 353-8 (1996) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8558460 | 11 | YM90K: pharmacological characterization as a selective and potent alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate/kainate receptor antagonist. | J Pharmacol Exp Ther 276: 84-92 (1996) | Yamanouchi Pharmaceutical Co., Ltd | 2D 3D TSV |
8558445 | 17 | Stable expression, pharmacologic properties and regulation of the human neuronal nicotinic acetylcholine alpha 4 beta 2 receptor. | J Pharmacol Exp Ther 276: 289-97 (1996) | Abbott Laboratories | 2D 3D TSV |
8549774 | 6 | Expression of functional mouse 5-HT5A serotonin receptor in the methylotrophic yeast Pichia pastoris: pharmacological characterization and localization. | FEBS Lett 377: 451-6 (1995) | Max-Planck-Institut | 2D 3D TSV |
8544178 | 46 | New alpha-thiol dipeptide dual inhibitors of angiotensin-I converting enzyme and neutral endopeptidase EC 3.4.24.11. | J Med Chem 38: 5023-30 (1996) | Ciba-Geigy Corporation | 2D 3D TSV |
8544176 | 16 | Identification, characterization and pharmacological profile of three metabolites of (R)-(+)-1,2,3,6-tetrahydro-4-phenyl-1-[(3-phenylcyclohexen-1- yl)methyl]pyridine (CI-1007), a dopamine autoreceptor agonist and potential antipsychotic agent. | J Med Chem 38: 5007-14 (1996) | Warner-Lambert Company | 2D 3D TSV |
8544175 | 75 | Synthesis, structure-affinity relationships, and biological activities of ligands binding to retinoic acid receptor subtypes. | J Med Chem 38: 4993-5006 (1996) | CIRD GALDERMA | 2D 3D TSV |
8544174 | 19 | Discovery of an orally bioavailable NK1 receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity. | J Med Chem 38: 4985-92 (1995) | GSK UK | 2D 3D TSV |
8544173 | 37 | Rational design and synthesis of small molecule, non-oligosaccharide selectin inhibitors: (alpha-D-mannopyranosyloxy)biphenyl-substituted carboxylic acids. | J Med Chem 38: 4976-84 (1996) | Texas Biotechnology Corporation | 2D 3D TSV |
8544172 | 3 | Introduction of a conformational switching element on a pyrrolidine ring. Synthesis and evaluation of (R*,R*)-(+/-)-methyl 3-acetyl-4-[3- (cyclopentyloxy)-4-methoxyphenyl]-3-methyl-1-pyrrolidinecarboxylate, a potent and selective inhibitor of cAMP-specific phosphodiesterase. | J Med Chem 38: 4972-5 (1996) | Glaxo Wellcome Research | 2D 3D TSV |
8544171 | 5 | Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors. | J Med Chem 38: 4968-71 (1995) | Upjohn | 2D 3D TSV |
8531090 | 1 | Pharmacological evaluation of 1229U91, a novel high-affinity and selective neuropeptide Y-Y1 receptor antagonist. | J Pharmacol Exp Ther 275: 1261-6 (1995) | Roche Bioscience | 2D 3D TSV |
8524985 | 69 | D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs. | Psychopharmacology (Berl) 120: 365-8 (1995) | Case Western Reserve University | 2D 3D TSV |
8523409 | 37 | 1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding. | J Med Chem 38: 4950-2 (1996) | Neurogen Corporation | 2D 3D TSV |
8523408 | 7 | The furoxan system as a useful tool for balancing"hybrids" with mixed alpha 1-antagonist and NO-like vasodilator activities. | J Med Chem 38: 4944-9 (1996) | Universit£ degli Studi di Torino | 2D 3D TSV |
8523406 | 59 | Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs. | J Med Chem 38: 4929-36 (1995) | Eli Lilly and Company | 2D 3D TSV |
8523405 | 176 | 3D-quantitative structure-activity relationships of human immunodeficiency virus type-1 proteinase inhibitors: comparative molecular field analysis of 2-heterosubstituted statine derivatives-implications for the design of novel inhibitors. | J Med Chem 38: 4917-28 (1996) | SANDOZ Forschungsinstitut Ges.m.b.H. | 2D 3D TSV |
8523403 | 50 | Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. | J Med Chem 38: 4897-905 (1996) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
8523400 | 26 | Nonsteroidal progesterone receptor ligands. 2. High-affinity ligands with selectivity for bone cell progesterone receptors. | J Med Chem 38: 4880-4 (1996) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
8523399 | 11 | Nonsteroidal progesterone receptor ligands. 1. 3-Aryl-1-benzoyl-1,4,5,6-tetrahydropyridazines. | J Med Chem 38: 4878-9 (1996) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
8522988 | 39 | Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. | J Neurochem 66: 47-56 (1996) | University of Washington | 2D 3D TSV |
8521788 | 22 | Molecular biology of somatostatin receptors. | Endocr Rev 16: 427-42 (1995) | University of Pennsylvania | 2D 3D TSV |
8515429 | 16 | (+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor. | J Med Chem 36: 1918-9 (1993) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8515428 | 2 | Enantioselectivity of cocaine recognition sites: binding of (1S)- and (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane (beta-CIT) to monoamine transporters. | J Med Chem 36: 1914-7 (1993) | Northeastern University | 2D 3D TSV |
8515427 | 43 | Multiple binding modes for the receptor-bound conformations of cyclic AII agonists. | J Med Chem 36: 1902-13 (1993) | Washington University | 2D 3D TSV |
8515426 | 12 | Inhibition and inactivation of presynaptic cholinergic markers using redox-reactive choline analogs. | J Med Chem 36: 1893-901 (1993) | University of Toledo | 2D 3D TSV |
8515425 | 65 | Potent nonpeptide angiotensin II receptor antagonists. 2. 1-(Carboxybenzyl)imidazole-5-acrylic acids. | J Med Chem 36: 1880-92 (1993) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8515423 | 26 | Structure-based design of inhibitors of purine nucleoside phosphorylase. 2. 9-Alicyclic and 9-heteroalicyclic derivatives of 9-deazaguanine. | J Med Chem 36: 1847-54 (1993) | BioCryst Pharmaceuticals Inc | 2D 3D TSV |
8515421 | 6 | The solution conformation of (D)Phe-Pro-containing peptides: implications on the activity of Ac-(D)Phe-Pro-boroArg-OH, a potent thrombin inhibitor. | J Med Chem 36: 1831-8 (1993) | DuPont Pharmaceuticals Company | 2D 3D TSV |
8515419 | 29 | 1,3,4-Oxadiazole, 1,3,4-thiadiazole, and 1,2,4-triazole analogs of the fenamates: in vitro inhibition of cyclooxygenase and 5-lipoxygenase activities. | J Med Chem 36: 1802-10 (1993) | Warner-Lambert Company | 2D 3D TSV |
8510101 | 37 | Nonpeptide angiotensin II receptor antagonists. 1. Synthesis and in vitro structure-activity relationships of 4-[[[(1H-pyrrol-1-ylacetyl)amino]phenyl]methyl]imidazole derivatives as angiotensin II receptor antagonists. | J Med Chem 36: 1735-45 (1993) | Warner-Lambert Company | 2D 3D TSV |
8510099 | 6 | Transformation of monoamine oxidase-B primary amine substrates into time-dependent inhibitors. Tertiary amine homologues of primary amine substrates. | J Med Chem 36: 1711-5 (1993) | Northwestern University | 2D 3D TSV |
8510008 | 67 | Species differences in the pharmacology of the 5-hydroxytryptamine2 receptor: structurally specific differentiation by ergolines and tryptamines. | J Pharmacol Exp Ther 265: 1272-9 (1993) | Eli Lilly and Company | 2D 3D TSV |
8496942 | 2 | Amidinium cation as a mimic of allylic carbocation: synthesis and squalene synthetase inhibitory activity of an amidinium analog of a carbocation intermediate. | J Med Chem 36: 631-2 (1993) | Sandoz Research Institute | 2D 3D TSV |
8496941 | 23 | 5-HT3 receptor antagonists. 2. 4-Hydroxy-3-quinolinecarboxylic acid derivatives. | J Med Chem 36: 617-26 (1993) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
8496939 | 100 | Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles. | J Med Chem 36: 591-609 (1993) | Merck Research Laboratories | 2D 3D TSV |
8496938 | 38 | Analogues of platelet activating factor. 8. Antagonists of PAF containing an aromatic ring linked to a pyridinium ring. | J Med Chem 36: 580-90 (1993) | American Cyanamid Company | 2D 3D TSV |
8496937 | 30 | Synthesis of 2-imidazolidinylidenepropanedinitrile derivatives as stimulators of gastrointestinal motility. | J Med Chem 36: 572-9 (1993) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
8496936 | 16 | Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites. | J Med Chem 36: 566-71 (1993) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8496935 | 25 | Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic agents. | J Med Chem 36: 544-51 (1993) | University of North Carolina | 2D 3D TSV |
8496932 | 72 | Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). 2. Modification of fatty acid anilide ACAT inhibitors: bioisosteric replacement of the amide bond. | J Med Chem 36: 1662-8 (1993) | Warner-Lambert Company | 2D 3D TSV |
8496931 | 152 | Structure-activity relationship of a series of phenylureas linked to 4-phenylimidazole. Novel potent inhibitors of acyl-CoA:cholesterol O-acyltransferase with antiatherosclerotic activity. 2. | J Med Chem 36: 1641-53 (1993) | Eisai Company, Ltd | 2D 3D TSV |
8496930 | 76 | Structure-activity relationship of N-[2-(dimethylamino)-6-[3-(5-methyl-4-phenyl-1H-imidazol-1-yl)propoxy] phenyl]-N'-pentylurea and analogues. Novel potent inhibitors of acyl-CoA:cholesterol O-acyltransferase with antiatherosclerotic activity. | J Med Chem 36: 1630-40 (1993) | Eisai Company, Ltd | 2D 3D TSV |
8496929 | 12 | Dibenzoxepin derivatives: thromboxane A2 synthase inhibition and thromboxane A2 receptor antagonism combined in one molecule. | J Med Chem 36: 1613-8 (1993) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
8496923 | 9 | New mechanism-based inactivators of trypsin-like proteinases. Selective inactivation of urokinase by functionalized cyclopeptides incorporating a sulfoniomethyl-substituted m-aminobenzoic acid residue. | J Med Chem 36: 1539-47 (1993) | CNRS-CERCOA | 2D 3D TSV |
8496922 | 92 | Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors. | J Med Chem 36: 1529-38 (1993) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
8496920 | 14 | (S)-N-tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors. | J Med Chem 36: 1509-10 (1993) | Wyeth Research (UK) | 2D 3D TSV |
8496919 | 15 | N-(arylalkyl)farnesylamines: new potent squalene synthetase inhibitors. | J Med Chem 36: 1501-4 (1993) | Sandoz Research Institute | 2D 3D TSV |
8496917 | 72 | Bridged gamma-carbolines and derivatives possessing selective and combined affinity for 5-HT2 and D2 receptors. | J Med Chem 36: 1488-95 (1993) | Scios Nova Inc | 2D 3D TSV |
8496909 | 4 | Mechanism-based inhibitors of prostaglandin omega-hydroxylase: (R)- and (S)-12-hydroxy-16-heptadecynoic acid and 2,2-dimethyl-12-hydroxy-16-heptadecynoic acid. | J Med Chem 36: 1418-24 (1993) | University of California | 2D 3D TSV |
8496908 | 39 | Interphenylene 7-oxabicyclo[2.2.1]heptane oxazoles. Highly potent, selective, and long-acting thromboxane A2 receptor antagonists. | J Med Chem 36: 1401-17 (1993) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8496907 | 8 | Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds. | J Med Chem 36: 1393-400 (1993) | Ciba-Geigy Ltd | 2D 3D TSV |
8496906 | 127 | Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position. | J Med Chem 36: 1380-6 (1993) | Hokuriku University | 2D 3D TSV |
8496905 | 6 | Synthesis and analgesic effects of N-[3-[(hydroxyamino) carbonyl]-1-oxo-2(R)-benzylpropyl]-L-isoleucyl-L-leucine, a new potent inhibitor of multiple neurotensin/neuromedin N degrading enzymes. | J Med Chem 36: 1369-79 (1993) | CCIPE-Faculté de Pharmacie | 2D 3D TSV |
8496902 | 139 | Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists. | J Med Chem 36: 1333-42 (1993) | National Institute of Diabetes | 2D 3D TSV |
8496900 | 136 | Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands. | J Med Chem 36: 1301-15 (1993) | Upjohn Laboratories | 2D 3D TSV |
8496821 | 2 | Pharmacological characterization of FK1052, a dihydropyridoindole derivative, as a new serotonin 3 and 4 dual receptor antagonist. | J Pharmacol Exp Ther 265: 752-8 (1993) | Fujisawa Pharmaceutical Co., Ltd | 2D 3D TSV |
8496700 | 16 | The Role of Receptor Binding in Drug Discovery | J Nat Prod 56: 441-455 (1993) | TBA | 2D 3D TSV |
8494379 | 4 | In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine. | Antimicrob Agents Chemother 37: 810-7 (1993) | National Cancer Institute-Bethesda | 2D 3D TSV |
8487261 | 27 | New nonpeptide angiotensin II receptor antagonists. 3. Synthesis, biological properties, and structure-activity relationships of 2-alkyl-4-(biphenylylmethoxy)pyridine derivatives. | J Med Chem 36: 1245-54 (1993) | Zeneca Pharmaceuticals | 2D 3D TSV |
8487257 | 57 | New indole derivatives as potent and selective serotonin uptake inhibitors. | J Med Chem 36: 1194-202 (1993) | Centre de Recherches de Vitry-Alfortville | 2D 3D TSV |
8487256 | 33 | Synthesis and structure-activity relationships of novel benzimidazole and imidazo[4,5-b]pyridine acid derivatives as thromboxane A2 receptor antagonists. | J Med Chem 36: 1175-87 (1993) | Carpibem | 2D 3D TSV |
8487255 | 84 | 5-[4-(benzyloxy)phenyl]-1,3,4-oxadiazol-2(3H)-one derivatives and related analogues: new reversible, highly potent, and selective monamine oxidase type B inhibitors. | J Med Chem 36: 1157-67 (1993) | Universit£ Paris 7 | 2D 3D TSV |
8487254 | 63 | Development of a pharmacophore for inhibition of human liver cytochrome P-450 2D6: molecular modeling and inhibition studies. | J Med Chem 36: 1136-45 (1993) | Institut f£r Toxikologie | 2D 3D TSV |
8478911 | 48 | Design and modeling of new platelet-activating factor antagonists. 1. Synthesis and biological activity of 1,4-bis(3',4',5'-trimethoxybenzoyl)-2-[[(substituted carbonyl and carbamoyl)oxy]methyl]piperazines. | J Med Chem 36: 990-1000 (1993) | Universit£ Paris 7 | 2D 3D TSV |
8478910 | 26 | Nonsymmetrical bipiperidyls as inhibitors of vesicular acetylcholine storage. | J Med Chem 36: 985-9 (1993) | University of Minnesota | 2D 3D TSV |
8478908 | 22 | Inhibitors of the protease from human immunodeficiency virus: synthesis, enzyme inhibition, and antiviral activity of a series of compounds containing the dihydroxyethylene transition-state isostere. | J Med Chem 36: 941-52 (1993) | Upjohn Laboratories | 2D 3D TSV |
8478906 | 25 | Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents. | J Med Chem 36: 1090-9 (1993) | Warner-Lambert Company | 2D 3D TSV |
8478905 | 53 | Inhibition studies of some serine and thiol proteinases by new leupeptin analogues. | J Med Chem 36: 1084-9 (1993) | University of Arkansas | 2D 3D TSV |
8478902 | 18 | Nucleosides. 5. Synthesis of guanine and formycin B derivatives as potential inhibitors of purine nucleoside phosphorylase. | J Med Chem 36: 1024-31 (1993) | National Defense Medical Center | 2D 3D TSV |
8474103 | 123 | Potent and selective inhibitors of an aspartyl protease-like endothelin converting enzyme identified in rat lung. | J Med Chem 36: 468-78 (1993) | Abbott Laboratories | 2D 3D TSV |
8474102 | 29 | Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3- [[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-L-alanine amide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (A-725 | J Med Chem 36: 460-7 (1993) | Abbott Laboratories | 2D 3D TSV |
8474101 | 30 | Studies directed toward the design of orally active renin inhibitors. 1. Some factors influencing the absorption of small peptides. | J Med Chem 36: 449-59 (1993) | Abbott Laboratories | 2D 3D TSV |
8474100 | 8 | Inactivation of monoamine oxidase B by analogues of the anticonvulsant agent milacemide (2-(n-pentylamino)acetamide). | J Med Chem 36: 446-8 (1993) | Northwestern University | 2D 3D TSV |
8474099 | 3 | Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile. | J Med Chem 36: 439-45 (1993) | Università di Firenze | 2D 3D TSV |
8474097 | 19 | Bicyclic compounds as ring-constrained inhibitors of protein-tyrosine kinase p56lck. | J Med Chem 36: 425-32 (1993) | National Cancer Institute-Bethesda | 2D 3D TSV |
8474008 | 58 | Cannabinoid structure-activity relationships: correlation of receptor binding and in vivo activities. | J Pharmacol Exp Ther 265: 218-26 (1993) | Virginia Commonwealth University | 2D 3D TSV |
8464047 | 14 | Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors. | J Med Chem 36: 924-7 (1993) | Merck Research Laboratories | 2D 3D TSV |
8464042 | 4 | Adenosine-5'-carboxaldehyde: a potent inhibitor of S-adenosyl-L-homocysteine hydrolase. | J Med Chem 36: 883-7 (1993) | University of Kansas | 2D 3D TSV |
8464040 | 21 | Substituted 3-phenyltropane analogs of cocaine: synthesis, inhibition of binding at cocaine recognition sites, and positron emission tomography imaging. | J Med Chem 36: 855-62 (1993) | Organix Inc | 2D 3D TSV |
8464039 | 12 | Synthesis and biodistribution of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate. A new ligand for the potential imaging of muscarinic receptors by single photon emission computed tomography. | J Med Chem 36: 848-54 (1993) | Oak Ridge National Laboratory | 2D 3D TSV |
8464038 | 14 | Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists. | J Med Chem 36: 842-7 (1993) | University of Toledo | 2D 3D TSV |
8461029 | 21 | Characterization of recombinant human serotonin 5HT1A receptors expressed in Chinese hamster ovary cells. [3H]spiperone discriminates between the G-protein-coupled and -uncoupled forms. | Biochem Pharmacol 45: 1003-9 (1993) | University of Canterbury | 2D 3D TSV |
8459400 | 74 | Design of thymidylate synthase inhibitors using protein crystal structures: the synthesis and biological evaluation of a novel class of 5-substituted quinazolinones. | J Med Chem 36: 733-46 (1993) | Agouron Pharmaceuticals Inc | 2D 3D TSV |
8459398 | 36 | 1,2-Cyclomethylenecarboxylic monoamide hydroxamic derivatives. A novel class of non-amino acid angiotensin converting enzyme inhibitors. | J Med Chem 36: 699-707 (1993) | Laboratori Guidotti S.p.A. | 2D 3D TSV |
8459396 | 37 | Centrally acting serotonergic agents. Synthesis and structure-activity relationships of C-1- or C-3-substituted derivatives of 8-hydroxy-2-(di-n-propylamino)tetralin. | J Med Chem 36: 671-82 (1993) | Upjohn Laboratories | 2D 3D TSV |
8450829 | 29 | Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization. | Mol Pharmacol 43: 313-9 (1993) | CNRS | 2D 3D TSV |
8437101 | 20 | Expression and characterization of the rat D3 dopamine receptor: pharmacologic properties and development of antibodies. | J Pharmacol Exp Ther 264: 1002-11 (1993) | University of Pennsylvania | 2D 3D TSV |
8426367 | 10 | 32-Methyl-32-oxylanosterols: dual-action inhibitors of cholesterol biosynthesis. | J Med Chem 36: 410-6 (1993) | Institute | 2D 3D TSV |
8426366 | 44 | Defining structural requirements for neuropeptide Y receptors using truncated and conformationally restricted analogues. | J Med Chem 36: 385-93 (1993) | Salk Institute | 2D 3D TSV |
8426364 | 30 | Inhibition of the tetracycline efflux antiport protein by 13-thio-substituted 5-hydroxy-6-deoxytetracyclines. | J Med Chem 36: 370-7 (1993) | Tufts University | 2D 3D TSV |
8426363 | 134 | Synthesis and in vitro evaluation of 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: high-affinity ligands for the N,N'-di-o-tolylguanidine-labeled sigma binding site. | J Med Chem 36: 343-52 (1993) | Scios Nova Inc | 2D 3D TSV |
8426362 | 46 | Symmetry-based inhibitors of HIV protease. Structure-activity studies of acylated 2,4-diamino-1,5-diphenyl-3-hydroxypentane and 2,5-diamino-1,6-diphenylhexane-3,4-diol. | J Med Chem 36: 320-30 (1993) | Abbott Laboratories | 2D 3D TSV |
8426361 | 111 | Highly selective tripeptide thrombin inhibitors. | J Med Chem 36: 314-9 (1993) | Eli Lilly and Company | 2D 3D TSV |
8426360 | 1 | Enantiospecific syntheses of alpha-(fluoromethyl)tryptophan analogues: interactions with tryptophan hydroxylase and aromatic L-amino acid decarboxylase. | J Med Chem 36: 305-13 (1993) | Mayo Clinic | 2D 3D TSV |
8424846 | 7 | LY248686, a new inhibitor of serotonin and norepinephrine uptake. | Neuropsychopharmacology 8: 23-33 (1993) | Eli Lilly and Company | 2D 3D TSV |
8423602 | 15 | Active site-directed synthetic thrombin inhibitors: synthesis, in vitro and in vivo activity profile of BMY 44621 and analogs. An examination of the role of the amino group in the D-Phe-Pro-Arg-H series. | J Med Chem 36: 300-3 (1993) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8423600 | 13 | 3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors. | J Med Chem 36: 292-4 (1993) | Merck Research Laboratories | 2D 3D TSV |
8423599 | 26 | Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere. | J Med Chem 36: 288-91 (1993) | Monsanto Corporate Research | 2D 3D TSV |
8423595 | 2 | (+)-Hemipalmitoylcarnitinium strongly inhibits carnitine palmitoyltransferase-I in intact mitochondria. | J Med Chem 36: 237-42 (1993) | Louisiana State University | 2D 3D TSV |
8423594 | 39 | Development of selective tight-binding inhibitors of leukotriene A4 hydrolase. | J Med Chem 36: 211-20 (1993) | Scripps Research Institute | 2D 3D TSV |
8423593 | 6 | Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 5. Synthesis and evaluation of enantiomers of 8-[[(4-chlorophenyl)sulfonyl]amino]-4-(3-pyridinylalkyl)octanoic acid. | J Med Chem 36: 205-10 (1993) | Ciba-Geigy Corporation | 2D 3D TSV |
8421294 | 5 | Structural determinants of haloenol lactone-mediated suicide inhibition of canine myocardial calcium-independent phospholipase A2. | J Med Chem 36: 95-100 (1993) | Washington University | 2D 3D TSV |
8421293 | 32 | Exploration of neutral endopeptidase active site by a series of new thiol-containing inhibitors. | J Med Chem 36: 87-94 (1993) | University of Paris | 2D 3D TSV |
8421291 | 73 | Structure-based design of inhibitors of purine nucleoside phosphorylase. 1. 9-(arylmethyl) derivatives of 9-deazaguanine. | J Med Chem 36: 55-69 (1993) | BioCryst Pharmaceuticals Inc | 2D 3D TSV |
8421290 | 46 | S-adenosylmethionine decarboxylase inhibitors: new aryl and heteroaryl analogues of methylglyoxal bis(guanylhydrazone). | J Med Chem 36: 46-54 (1993) | Ciba-Geigy AG | 2D 3D TSV |
8421286 | 44 | Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction. | J Med Chem 36: 21-9 (1993) | Roche Products Limited | 2D 3D TSV |
8421285 | 12 | Hemicholinium and related lipids: inhibitors of protein kinase C. | J Med Chem 36: 177-8 (1993) | Louisiana State University | 2D 3D TSV |
8421284 | 7 | Phosphorus-containing inhibitors of endothelin converting enzyme: effects of the electronic nature of phosphorus on inhibitor potency. | J Med Chem 36: 173-6 (1993) | Monsanto Corp | 2D 3D TSV |
8421283 | 43 | CCK-B agonist or antagonist activities of structurally hindered and peptidase-resistant Boc-CCK4 derivatives. | J Med Chem 36: 166-72 (1993) | University of Paris | 2D 3D TSV |
8421282 | 22 | Synthesis and structure-activity relationship of some 5-[[[(dialkylamino)alkyl]-1-piperidinyl]acetyl]-10,11-dihydro-5H- benzo[b,e][1,4]diazepin-11-ones as M2-selective antimuscarinics. | J Med Chem 36: 162-5 (1993) | George Washington University Medical Center | 2D 3D TSV |
8421274 | 27 | Nonpeptide angiotensin II antagonists: N-phenyl-1H-pyrrole derivatives are angiotensin II receptor antagonists. | J Med Chem 36: 101-10 (1993) | Searle & Company | 2D 3D TSV |
8413837 | 45 | [3H]paroxetine binding in rat frontal cortex strongly correlates with [3H]5-HT uptake: effect of administration of various antidepressant treatments. | Neuropharmacology 32: 737-43 (1993) | Boots Pharmaceuticals | 2D 3D TSV |
8411022 | 9 | Deoxygenated inositol 1,4,5-trisphosphate analogues and their interaction with metabolic enzymes. (1R,2R,4R)-cyclohexane-1,2,4-tris(methylenesulfonate): a potent selective 5-phosphatase inhibitor. | J Med Chem 36: 3035-8 (1993) | Mayo Foundation | 2D 3D TSV |
8411021 | 3 | Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor. | J Med Chem 36: 3032-4 (1993) | Hebrew University | 2D 3D TSV |
8411020 | 2 | N-(carboxymethyl)-N-[3,5-bis(decyloxy)-phenyl]glycine (Ro 23-9358): a potent inhibitor of secretory phospholipases A2 with antiinflammatory activity. | J Med Chem 36: 3029-31 (1993) | Roche Research Center | 2D 3D TSV |
8411019 | 6 | Hydroxylated 2-(5'-salicyl)naphthalenes as protein-tyrosine kinase inhibitors. | J Med Chem 36: 3015-20 (1993) | National Institutes of Health | 2D 3D TSV |
8411018 | 6 | Inhibition of herpes simplex virus type 1 ribonucleotide reductase by substituted tetrapeptide derivatives. | J Med Chem 36: 3005-9 (1993) | Bio-M£ga/Boehringer Ingelheim Research Inc. | 2D 3D TSV |
8411016 | 76 | Synthesis and structure-activity relationships of 1-acyl-4-((2-methyl-3-pyridyl)cyanomethyl)piperazines as PAF antagonists. | J Med Chem 36: 2984-97 (1993) | J. Uriach & Cía. S.A. | 2D 3D TSV |
8411014 | 20 | Imidazol-1-yl and pyridin-3-yl derivatives of 4-phenyl-1,4-dihydropyridines combining Ca2+ antagonism and thromboxane A2 synthase inhibition. | J Med Chem 36: 2964-72 (1993) | Farmitalia Carlo Erba | 2D 3D TSV |
8411012 | 19 | Synthesis and protein-tyrosine kinase inhibitory activity of polyhydroxylated stilbene analogues of piceatannol. | J Med Chem 36: 2950-5 (1993) | Purdue University | 2D 3D TSV |
8411011 | 23 | Inhibitors of acyl-CoA:cholesterol acyltransferase. 5. Identification and structure-activity relationships of novel beta-ketoamides as hypocholesterolemic agents. | J Med Chem 36: 2943-9 (1993) | Warner-Lambert Company | 2D 3D TSV |
8411007 | 392 | Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. | J Med Chem 36: 2908-20 (1993) | Mayo Foundation | 2D 3D TSV |
8411005 | 42 | 2-Amido-8-methoxytetralins: a series of nonindolic melatonin-like agents. | J Med Chem 36: 2891-8 (1993) | University of Groningen | 2D 3D TSV |
8411004 | 48 | 3-Aryl-2-(3'-substituted-1',2',4'-oxadiazol-5'-yl)tropane analogues of cocaine: affinities at the cocaine binding site at the dopamine, serotonin, and norepinephrine transporters. | J Med Chem 36: 2886-90 (1993) | Research Triangle Institute | 2D 3D TSV |
8411003 | 12 | A structure-activity study of four dopamine D-1 and D-2 receptor antagonists, representing the phenylindan, -indene, and -indole structural classes of compounds. | J Med Chem 36: 2878-85 (1993) | University of Lund | 2D 3D TSV |
8411002 | 67 | Cholecystokinin peptidomimetics as selective CCK-B antagonists: design, synthesis, and in vitro and in vivo biochemical properties. | J Med Chem 36: 2868-77 (1993) | University of Paris | 2D 3D TSV |
8410999 | 81 | 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. | J Med Chem 36: 2842-50 (1993) | Eli Lilly and Company | 2D 3D TSV |
8410998 | 129 | Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors. | J Med Chem 36: 2833-41 (1993) | Eli Lilly and Company | 2D 3D TSV |
8410995 | 18 | Synthesis and evaluation of a series of benzylaniline hydrochlorides as potential cytotoxic and antimitotic agents acting by inhibition of tubulin polymerization. | J Med Chem 36: 2817-21 (1993) | Purdue University | 2D 3D TSV |
8410993 | 24 | Mammalian topoisomerase II inhibitory activity of 1-cyclopropyl-6,8- difluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinolinecarb oxylic acid and related derivatives. | J Med Chem 36: 2801-9 (1993) | Sterling Winthrop Pharmaceuticals Research Division | 2D 3D TSV |
8410992 | 35 | Renin inhibitors containing a pyridyl amino diol derived C-terminus. | J Med Chem 36: 2788-800 (1993) | Hoechst AG | 2D 3D TSV |
8410991 | 88 | Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation of L-691,816. | J Med Chem 36: 2771-87 (1993) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
8410990 | 141 | Stereospecific and selective 5-HT2 antagonism in a series of 5-substituted trans-1-piperazino-3-phenylindans. | J Med Chem 36: 2761-70 (1993) | H. Lundbeck A/S | 2D 3D TSV |
8410989 | 58 | Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents. | J Med Chem 36: 2751-60 (1993) | Solvay Duphar Research Laboratories | 2D 3D TSV |
8410988 | 12 | Novel antagonists of 5-HT3 receptors. Synthesis and biological evaluation of piperazinylquinoxaline derivatives. | J Med Chem 36: 2745-50 (1993) | Universidad de Navarra | 2D 3D TSV |
8410983 | 7 | (E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid: a novel high-affinity leukotriene B4 receptor antagonist. | J Med Chem 36: 2703-5 (1993) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8410982 | 5 | Keto/enol epoxy steroids: a new structural class of HIV-1 Tat inhibitors. | J Med Chem 36: 2701-2 (1993) | Sterling Winthrop Pharmaceuticals Research Division | 2D 3D TSV |
8410981 | 63 | Plant antitumor agents. 30. Synthesis and structure activity of novel camptothecin analogs. | J Med Chem 36: 2689-700 (1993) | Research Triangle Institute | 2D 3D TSV |
8410980 | 8 | 2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists. | J Med Chem 36: 2676-88 (1993) | Abbott Laboratories | 2D 3D TSV |
8410977 | 43 | 2-(Quinuclidin-3-yl)pyrido[4,3-b]indol-1-ones and isoquinolin-1-ones. Potent conformationally restricted 5-HT3 receptor antagonists. | J Med Chem 36: 2645-57 (1993) | Syntex Research | 2D 3D TSV |
8410976 | 60 | Effect of trifluoromethyl and other substituents on activity of xanthines at adenosine receptors. | J Med Chem 36: 2639-44 (1993) | National Institutes of Health | 2D 3D TSV |
8410973 | 75 | Specificity in the binding of inhibitors to the active site of human/primate aspartic proteinases: analysis of P2-P1-P1'-P2' variation. | J Med Chem 36: 2614-20 (1993) | University of Florida | 2D 3D TSV |
8410972 | 52 | Conformational effects on retinoid receptor selectivity. 1. Effect of 9-double bond geometry on retinoid X receptor activity. | J Med Chem 36: 2605-13 (1993) | SRI International | 2D 3D TSV |
8410970 | 106 | Structure-activity relationships of C-terminal endothelin hexapeptide antagonists. | J Med Chem 36: 2585-94 (1993) | Warner-Lambert Company | 2D 3D TSV |
8398139 | 29 | A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms. | Neuron 11: 449-58 (1993) | The Scripps Research Institute | 2D 3D TSV |
8397408 | 27 | Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation. | Proc Natl Acad Sci U S A 90: 8547-51 (1993) | U. 109 | 2D 3D TSV |
8396931 | 11 | Cloning, functional expression and tissue distribution of human cDNA for the alpha 1C-adrenergic receptor. | Biochem Biophys Res Commun 195: 902-9 (1993) | National Children's Medical Research Center | 2D 3D TSV |
8394987 | 32 | Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase. | Mol Pharmacol 44: 229-36 (1993) | CNRS | 2D 3D TSV |
8394936 | 11 | Design of potent non-peptide competitive antagonists of the human bradykinin B2 receptor. | J Med Chem 36: 2583-4 (1993) | Sterling Winthrop Pharmaceutical Research Division | 2D 3D TSV |
8394935 | 4 | A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists. | J Med Chem 36: 2572-4 (1993) | University of Minnesota | 2D 3D TSV |
8394934 | 9 | Design of potent, cyclic peptide bradykinin receptor antagonists from conformationally constrained linear peptides. | J Med Chem 36: 2569-71 (1993) | Scios Nova Inc | 2D 3D TSV |
8394902 | 11 | Imidazenil: a new partial positive allosteric modulator of gamma-aminobutyric acid (GABA) action at GABAA receptors. | J Pharmacol Exp Ther 266: 1018-28 (1993) | Georgetown University | 2D 3D TSV |
8394362 | 99 | Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype. | J Biol Chem 268: 18200-4 (1993) | National Institute of Neurological Disorders and Stroke | 2D 3D TSV |
8393489 | 25 | A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines. | J Med Chem 36: 2075-83 (1993) | Glaxo Group Research Ltd. | 2D 3D TSV |
8393115 | 11 | N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists. | J Med Chem 36: 2044-5 (1993) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
8393113 | 114 | Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone. | J Med Chem 36: 2011-7 (1993) | Otsuka Pharmaceutical Co., Ltd | 2D 3D TSV |
8393112 | 12 | Quinolone antibacterials: synthesis and biological activity of carbon isosteres of the 1-piperazinyl and 3-amino-1-pyrrolidinyl side chains. | J Med Chem 36: 1964-70 (1993) | Warner-Lambert Company | 2D 3D TSV |
8391122 | 35 | Cloning of cDNA sequences encoding human alpha 2 and alpha 3 gamma-aminobutyric acidA receptor subunits and characterization of the benzodiazepine pharmacology of recombinant alpha 1-, alpha 2-, alpha 3-, and alpha 5-containing human gamma-aminobutyric acidA receptors. | Mol Pharmacol 43: 970-5 (1993) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
8390575 | 28 | Non-peptide ligands for opioid receptors. Design of kappa-specific agonists. | J Med Chem 36: 1860-5 (1993) | Universit£ di Catania | 2D 3D TSV |
8389876 | 11 | Design, synthesis, and pharmacological evaluation of potent xanthone dicarboxylic acid leukotriene B4 receptor antagonists. | J Med Chem 36: 1726-34 (1993) | Eli Lilly and Company | 2D 3D TSV |
8389875 | 34 | Antitumor agents. 3. Synthesis and biological activity of 4 beta-alkyl derivatives containing hydroxy, amino, and amido groups of 4'-O-demethyl-4-desoxypodophyllotoxin as antitumor agents. | J Med Chem 36: 1689-99 (1993) | Taiho Pharmaceutical Co., Ltd | 2D 3D TSV |
8388471 | 28 | Tetrapeptide tachykinin antagonists: synthesis and modulation of the physicochemical and pharmacological properties of a new series of partially cyclic analogs. | J Med Chem 36: 1654-61 (1993) | Institut de Recherches Servier | 2D 3D TSV |
8388469 | 3 | NMR and computational evidence that high-affinity bradykinin receptor antagonists adopt C-terminal beta-turns. | J Med Chem 36: 1450-60 (1993) | Scios Nova Inc | 2D 3D TSV |
8388468 | 37 | Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase. | J Med Chem 36: 1387-92 (1993) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8388466 | 15 | Amino- and guanidinoacylryanodines: basic ryanodine esters with enhanced affinity for the sarcoplasmic reticulum Ca(2+)-release channel. | J Med Chem 36: 1319-23 (1993) | Indiana University | 2D 3D TSV |
8387599 | 1 | Synthesis and phosphodiesterase activity of carboxylic acid mimetics of cyclic guanosine 3',5'-monophosphate. | J Med Chem 36: 1210-20 (1993) | Schering-Plough Research Institute | 2D 3D TSV |
8387598 | 11 | Synthesis and cytotoxicity of 1,6,7,8-substituted 2-(4'-substituted phenyl)-4-quinolones and related compounds: identification as antimitotic agents interacting with tubulin. | J Med Chem 36: 1146-56 (1993) | Institute of Pharmaceutical Chemistry | 2D 3D TSV |
8387597 | 3 | Bioactive ryanoids from nucleophilic additions to 4,12-seco-4,12-dioxoryanodine. | J Med Chem 36: 1128-35 (1993) | University of California | 2D 3D TSV |
8386236 | 11 | In vitro and in vivo pharmacological characterization of N6-cyclopentyl-9-methyladenine (N-0840): a selective, orally active A1 adenosine receptor antagonist. | J Pharmacol Exp Ther 265: 227-36 (1993) | Whitby Research, Inc. | 2D 3D TSV |
8385226 | 7 | The effect of NMeTyr5 substitution in luteinizing hormone-releasing hormone antagonists. | J Med Chem 36: 928-33 (1993) | Abbott Laboratories | 2D 3D TSV |
8385225 | 16 | Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy. | J Med Chem 36: 871-82 (1993) | Warner-Lambert Company | 2D 3D TSV |
8385224 | 9 | Synthesis and anti-HIV evaluation of D4T and D4T 5'-monophosphate prodrugs. | J Med Chem 36: 826-30 (1993) | URA CNRS 1309 | 2D 3D TSV |
8384716 | 6 | Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes. | Proc Natl Acad Sci U S A 90: 2184-8 (1993) | The Scripps Research Institute | 2D 3D TSV |
8384662 | 20 | A topochemical approach to explain morphiceptin bioactivity. | J Med Chem 36: 708-19 (1993) | University of California | 2D 3D TSV |
8383731 | 2 | A new bastadin from the sponge Psammaplysilla purpurea. | J Nat Prod 56: 153-7 (1993) | University of Hawaii | 2D 3D TSV |
8383730 | 7 | New Leukotriene B4 Receptor Antagonist: Leucettamine A and Related Imidazole Alkaloids from the Marine Sponge Leucetta microraphis | J Nat Prod 56: 116-121 (1993) | TBA | 2D 3D TSV |
8382063 | 12 | Activity of serotonin (5-HT) receptor agonists, partial agonists and antagonists at cloned human 5-HT1A receptors that are negatively coupled to adenylate cyclase in permanently transfected HeLa cells. | Biochem Pharmacol 45: 375-83 (1993) | Janssen Research Foundation | 2D 3D TSV |
8381185 | 24 | Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase. | J Med Chem 36: 421-3 (1993) | Eli Lilly and Company | 2D 3D TSV |
8381184 | 42 | Substituted 3-(phenylmethyl)-1H-indole-5-carboxamides and 1-(phenylmethyl)indole-6-carboxamides as potent, selective, orally active antagonists of the peptidoleukotrienes. | J Med Chem 36: 394-409 (1993) | ICI Pharmaceuticals Group | 2D 3D TSV |
8381183 | 35 | Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists. | J Med Chem 36: 363-9 (1993) | Abbott Laboratories | 2D 3D TSV |
8380639 | 24 | Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. | Proc Natl Acad Sci U S A 90: 408-12 (1993) | Synaptic Pharmaceutical Corporation | 2D 3D TSV |
8380614 | 6 | A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists. | J Med Chem 36: 179-80 (1993) | University of Minnesota | 2D 3D TSV |
8377012 | 2 | Polycyclic guanidine alkaloids from the marine sponge Crambe crambe and Ca++ channel blocker activity of crambescidin 816. | J Nat Prod 56: 1007-15 (1993) | University of Brussels | 2D 3D TSV |
8360888 | 14 | Application of a conformationally restricted Phe-Leu dipeptide mimetic to the design of a combined inhibitor of angiotensin I-converting enzyme and neutral endopeptidase 24.11. | J Med Chem 36: 2420-3 (1993) | Marion Merrell Dow Research Institute | 2D 3D TSV |
8360887 | 9 | Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity. | J Med Chem 36: 2412-5 (1993) | University of Minnesota | 2D 3D TSV |
8360886 | 4 | A mechanism-based inactivation study of neutral endopeptidase 24.11. | J Med Chem 36: 2408-11 (1993) | Salk Biotechnology/Industrial Associates | 2D 3D TSV |
8360884 | 134 | Three-dimensional quantitative structure-activity relationship of angiotesin-converting enzyme and thermolysin inhibitors. II. A comparison of CoMFA models incorporating molecular orbital fields and desolvation free energies based on active-analog and complementary-receptor-field alignment rules. | J Med Chem 36: 2390-403 (1993) | Washington University | 2D 3D TSV |
8360883 | 49 | Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 3. The hydrophobic side-chain"C-region". | J Med Chem 36: 2381-9 (1993) | Sandoz Institute for Medical Research | 2D 3D TSV |
8360882 | 30 | Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 2. The amide bond"B-region". | J Med Chem 36: 2373-80 (1993) | Sandoz Institute for Medical Research | 2D 3D TSV |
8360878 | 29 | Quinoxaline N-oxide containing potent angiotensin II receptor antagonists: synthesis, biological properties, and structure-activity relationships. | J Med Chem 36: 2335-42 (1993) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8360876 | 9 | A novel constrained reduced-amide inhibitor of HIV-1 protease derived from the sequential incorporation of gamma-turn mimetics into a model substrate. | J Med Chem 36: 2321-31 (1993) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8360875 | 23 | Synthesis and evaluation of conformationally restricted N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamines at sigma receptors. 2. Piperazines, bicyclic amines, bridged bicyclic amines, and miscellaneous compounds. | J Med Chem 36: 2311-20 (1993) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8360874 | 19 | Potent HIV protease inhibitors: the development of tetrahydrofuranylglycines as novel P2-ligands and pyrazine amides as P3-ligands. | J Med Chem 36: 2300-10 (1993) | Merck Research Laboratories | 2D 3D TSV |
8360873 | 25 | Synthesis and structure-activity studies of a series of spirooxazolidine-2,4-diones: 4-oxa analogues of the muscarinic agonist 2-ethyl-8-methyl-2,8-diazaspiro[4.5]decane-1,3-dione. | J Med Chem 36: 2292-9 (1993) | Institute for Drug Discovery Research | 2D 3D TSV |
8360872 | 3 | Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some 3-amino- and 3-methylbenzo[f]quinazolin-1(2H)-ones. | J Med Chem 36: 2279-91 (1993) | Wellcome Research Laboratories | 2D 3D TSV |
8360871 | 86 | Nonpeptide angiotensin II receptor antagonists. 2. Design, synthesis, and structure-activity relationships of 2-alkyl-4-(1H-pyrrol-1-yl)-1H-imidazole derivatives: profile of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)-[1,1' -biphenyl]-4-yl]-methyl]-4-[2-(trifluoroacetyl)-1H-pyrrol-1-yl]-1H- imidazole-5-car | J Med Chem 36: 2253-65 (1993) | Warner-Lambert Company | 2D 3D TSV |
8358562 | 29 | Development of a radioligand binding assay for 5-HT4 receptors in guinea-pig and rat brain. | Br J Pharmacol 109: 618-24 (1993) | Glaxo Group Research Ltd. | 2D 3D TSV |
8355256 | 11 | Peptidomimetic HIV protease inhibitors: phosphate prodrugs with improved biological activities. | J Med Chem 36: 2575-7 (1993) | Upjohn Company | 2D 3D TSV |
8355255 | 103 | Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones. | J Med Chem 36: 2558-68 (1993) | Merck Research Laboratories | 2D 3D TSV |
8355253 | 74 | Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist. | J Med Chem 36: 2519-25 (1993) | Virginia Commonwealth University | 2D 3D TSV |
8355252 | 54 | Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance. | J Med Chem 36: 2508-18 (1993) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
8355251 | 8 | Synthesis and binding properties of MK-801 isothiocyanates; (+)-3-isothiocyanato-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten- 5,10-imine hydrochloride: a new, potent and selective electrophilic affinity ligand for the NMDA receptor-coupled phencyclidine binding site. | J Med Chem 36: 2499-507 (1993) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8355247 | 34 | Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2'-dithiobis(1H-indole-3-alkanoic acids). | J Med Chem 36: 2459-69 (1993) | University of Auckland | 2D 3D TSV |
8355245 | 18 | Activated ketone based inhibitors of human renin. | J Med Chem 36: 2431-47 (1993) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8340925 | 18 | Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. | J Med Chem 36: 2235-7 (1993) | Syntex Discovery Research | 2D 3D TSV |
8340923 | 7 | Synthesis and antitumor activity of 10-propargyl-10-deazaaminopterin. | J Med Chem 36: 2228-31 (1993) | SRI International | 2D 3D TSV |
8340922 | 7 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. | J Med Chem 36: 2208-18 (1993) | Upjohn Laboratories | 2D 3D TSV |
8340921 | 43 | Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazolecarboxylic acids. | J Med Chem 36: 2182-95 (1993) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
8340920 | 43 | Synthesis and structure-activity relationships of nonpeptide, potent triazolone-based angiotensin II receptor antagonists. | J Med Chem 36: 2172-81 (1993) | Searle R&D | 2D 3D TSV |
8340919 | 4 | 4-Amidinoindan-1-one 2'-amidinohydrazone: a new potent and selective inhibitor of S-Adenosylmethionine decarboxylase. | J Med Chem 36: 2168-71 (1993) | Ciba-Geigy AG | 2D 3D TSV |
8340918 | 4 | Multiple copy simultaneous search and construction of ligands in binding sites: application to inhibitors of HIV-1 aspartic proteinase. | J Med Chem 36: 2142-67 (1993) | Harvard University | 2D 3D TSV |
8340917 | 19 | Sulfonylmethanesulfonamide inhibitors of carbonic anhydrase. | J Med Chem 36: 2134-41 (1993) | Merck Research Laboratories | 2D 3D TSV |
8340910 | 32 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. | J Med Chem 36: 2059-65 (1993) | University of Göteborg | 2D 3D TSV |
8340909 | 14 | Excursions in drug discovery. | J Med Chem 36: 2051-8 (1993) | Merck Research Laboratories | 2D 3D TSV |
8336341 | 42 | Synthesis and biological evaluation of antiplatelet 2-aminochromones. | J Med Chem 36: 2026-32 (1993) | Upjohn Laboratories | 2D 3D TSV |
8335064 | 4 | Characteristics of histamine H1 receptors on HeLa cells. | Eur J Pharmacol 245: 291-5 (1993) | University of Cambridge | 2D 3D TSV |
8326323 | 7 | Microbial transformation of L-696,474, a novel cytochalasin as an inhibitor of HIV-1 protease. | J Nat Prod 56: 755-61 (1993) | Merck Research Laboratories | 2D 3D TSV |
8308869 | 5 | Selective protection and relative importance of the carboxylic acid groups of zaragozic acid A for squalene synthase inhibition. | J Med Chem 37: 421-4 (1994) | Merck Research Laboratories | 2D 3D TSV |
8308867 | 72 | Synthesis of high specific activity [3H]-9-cis-retinoic acid and its application for identifying retinoids with unusual binding properties. | J Med Chem 37: 408-14 (1994) | Ligand Pharmaceuticals Inc | 2D 3D TSV |
8308865 | 9 | CNAD: a potent and specific inhibitor of alcohol dehydrogenase. | J Med Chem 37: 392-9 (1994) | University of Rochester Medical Center | 2D 3D TSV |
8308857 | 19 | The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide. | J Med Chem 37: 329-31 (1994) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8302837 | 4 | Bound water molecules and conformational stabilization help mediate an antigen-antibody association. | Proc Natl Acad Sci USA 91: 1089-93 (1994) | Institut Pasteur | 2D 3D TSV |
8302271 | 63 | Pharmacological heterogeneity of the cloned and native human dopamine transporter: disassociation of [3H]WIN 35,428 and [3H]GBR 12,935 binding. | Mol Pharmacol 45: 125-35 (1994) | University of Toronto | 2D 3D TSV |
8301592 | 45 | Pharmacological and functional characterization of D2, D3 and D4 dopamine receptors in fibroblast and dopaminergic cell lines. | J Pharmacol Exp Ther 268: 495-502 (1994) | Washington University | 2D 3D TSV |
8301582 | 57 | Expression and pharmacological characterization of the human D3 dopamine receptor. | J Pharmacol Exp Ther 268: 417-26 (1994) | Neuroscience Research Centre | 2D 3D TSV |
8301575 | 55 | Novel benzodioxopiperazines acting as antagonists at postsynaptic 5-HT1A receptors and as agonists at 5-HT1A autoreceptors: a comparative pharmacological characterization with proposed 5-HT1A antagonists. | J Pharmacol Exp Ther 268: 337-52 (1994) | Institut de Recherches Servier | 2D 3D TSV |
8295221 | 28 | Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity. | J Med Chem 37: 322-8 (1994) | Warner-Lambert Company | 2D 3D TSV |
8295220 | 18 | A new approach to the design of sigma-2-selective ligands: synthesis and evaluation of N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1- pyrrolidinyl)ethylamine-related polyamines at sigma-1 and sigma-2 receptor subtypes. | J Med Chem 37: 314-21 (1994) | National Institutes of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8295219 | 44 | Tetrapeptide CCK agonists: structure-activity studies on modifications at the N-terminus. | J Med Chem 37: 309-13 (1994) | Abbott Laboratories | 2D 3D TSV |
8295218 | 3 | Adenosine deaminase inhibitors. Synthesis and biological evaluation of 4-amino-1-(2(S)-hydroxy-3(R)-nonyl)-1H-imidazo[4,5-c]pyridine (3-deaza-(+)-EHNA) and certain C1' derivatives. | J Med Chem 37: 305-8 (1994) | University of Rhode Island | 2D 3D TSV |
8295217 | 7 | Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors. | J Med Chem 37: 293-304 (1994) | Upjohn Laboratories | 2D 3D TSV |
8295214 | 21 | Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers. | J Med Chem 37: 268-74 (1994) | Warner-Lambert Company | 2D 3D TSV |
8295213 | 59 | Synthesis and structure-activity studies of N,N'-diarylguanidine derivatives. N-(1-naphthyl)-N'-(3-ethylphenyl)-N'-methylguanidine: a new, selective noncompetitive NMDA receptor antagonist. | J Med Chem 37: 260-7 (1994) | Cambridge NeuroScience Inc | 2D 3D TSV |
8295212 | 31 | Novel cAMP PDE III inhibitors: imidazo[4,5-b]pyridin-2(3H)-ones and thiazolo[4,5-b]pyridin-2(3H)-ones and their analogs. | J Med Chem 37: 248-54 (1994) | Sterling Winthrop Pharmaceuticals Research Division | 2D 3D TSV |
8295211 | 35 | 3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors. | J Med Chem 37: 240-7 (1994) | Merck Research Laboratories | 2D 3D TSV |
8295207 | 2 | Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential. | J Med Chem 37: 219-21 (1994) | University of Bath | 2D 3D TSV |
8295206 | 6 | Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin. Evidence for improved transport. | J Med Chem 37: 215-8 (1994) | University of Pennsylvania | 2D 3D TSV |
8289207 | 30 | Mixed 5-HT1A/D-2 activity of a new model of arylpiperazines: 1-aryl-4-[3-(1,2-dihydronaphthalen-4-yl)-n-propyl]piperazines. 1. Synthesis and structure-activity relationships. | J Med Chem 37: 99-104 (1994) | Università di Bari | 2D 3D TSV |
8289199 | 105 | 6,6-Disubstituted Hex-5-enoic acid derivatives as combined thromboxane A2 receptor antagonists and synthetase inhibitors. | J Med Chem 37: 26-39 (1994) | Dr. Karl Thomae GmbH | 2D 3D TSV |
8289198 | 53 | A recombinant human stromelysin catalytic domain identifying tryptophan derivatives as human stromelysin inhibitors. | J Med Chem 37: 206-9 (1994) | Warner-Lambert Company | 2D 3D TSV |
8289197 | 20 | Adenosine deaminase inhibitors: synthesis and structure-activity relationships of 2-hydroxy-3-nonyl derivatives of azoles. | J Med Chem 37: 201-5 (1994) | Universit£ di Camerino | 2D 3D TSV |
8289196 | 7 | New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C. | J Med Chem 37: 195-200 (1994) | University of North Carolina | 2D 3D TSV |
8289195 | 28 | Isozyme-specific glutathione-S-transferase inhibitors: design and synthesis. | J Med Chem 37: 189-94 (1994) | Terrapin Technologies | 2D 3D TSV |
8289190 | 31 | Synthesis of novel N-phosphonoalkyl dipeptide inhibitors of human collagenase. | J Med Chem 37: 158-69 (1994) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8289189 | 1 | Interaction of tetrahydrostilbazoles with monoamine oxidase A and B. | J Med Chem 37: 151-7 (1994) | University of California | 2D 3D TSV |
8289188 | 30 | Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors. | J Med Chem 37: 146-50 (1994) | University of Arizona | 2D 3D TSV |
8289187 | 47 | Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors. | J Med Chem 37: 141-5 (1994) | University of Arizona | 2D 3D TSV |
8289184 | 45 | Conformational analysis of 5-lipoxygenase inhibitors: role of the substituents in chiral recognition and on the active conformations of the (methoxyalkyl)thiazole and methoxytetrahydropyran series. | J Med Chem 37: 113-24 (1994) | AstraZeneca | 2D 3D TSV |
8289183 | 24 | Synthesis and structure activity relationships of cis- and trans-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines for 5-HT receptor subtypes. | J Med Chem 37: 105-12 (1994) | Abbott Laboratories | 2D 3D TSV |
8289063 | 5 | Zaragozic Acids D and D2: Potent Inhibitors of Squalene Synthase and of Ras Farnesyl-Protein Transferase | J Nat Prod 56: 1923-1929 (1993) | TBA | 2D 3D TSV |
8278895 | 52 | Evaluation of 5-[18F]fluoropropylepidepride as a potential PET radioligand for imaging dopamine D2 receptors. | Synapse 15: 169-76 (1993) | Vanderbilt University | 2D 3D TSV |
8277514 | 46 | 6-Azasteroids: potent dual inhibitors of human type 1 and 2 steroid 5 alpha-reductase. | J Med Chem 36: 4313-5 (1994) | Glaxo Inc. Research Institute | 2D 3D TSV |
8277513 | 4 | Synthesis and optical resolution of (R)- and (S)-trans-7-Hydroxy-2-[N-propyl-N-(3'-iodo-2'-propenyl)amino]tetralin: a new D3 dopamine receptor ligand. | J Med Chem 36: 4308-12 (1994) | University of Pennsylvania | 2D 3D TSV |
8277511 | 57 | Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides. | J Med Chem 36: 4293-301 (1994) | Merck Research Laboratories | 2D 3D TSV |
8277510 | 233 | Development of 1,4-benzodiazepine cholecystokinin type B antagonists. | J Med Chem 36: 4276-92 (1994) | Merck Research Laboratories | 2D 3D TSV |
8277506 | 58 | Non-peptide angiotensin II receptor antagonists. 2. Design, synthesis, and biological activity of N-substituted (phenylamino)phenylacetic acids and acyl sulfonamides. | J Med Chem 36: 4239-49 (1994) | Merck Research Laboratories | 2D 3D TSV |
8277505 | 58 | Non-peptide angiotensin II receptor antagonists. 1. Design, synthesis, and biological activity of N-substituted indoles and dihydroindoles. | J Med Chem 36: 4230-8 (1994) | Merck Research Laboratories | 2D 3D TSV |
8277497 | 17 | Studies on analogues of classical antifolates bearing the naphthoyl group in place of benzoyl in the side chain. | J Med Chem 36: 4161-71 (1994) | Southern Research Institute | 2D 3D TSV |
8277496 | 77 | Three-dimensional QSAR of human immunodeficiency virus (I) protease inhibitors. 1. A CoMFA study employing experimentally-determined alignment rules. | J Med Chem 36: 4152-60 (1994) | Washington University | 2D 3D TSV |
8277318 | 7 | Kinase inhibitors from Polygonum cuspidatum. | J Nat Prod 56: 1805-10 (1993) | Purdue University | 2D 3D TSV |
8263508 | 9 | Molecular cloning, expression, and pharmacological characterization of humEAA1, a human kainate receptor subunit. | J Neurochem 62: 1-9 (1994) | Allelix Biopharmaceuticals, Inc. | 2D 3D TSV |
8258837 | 8 | (1-Butyl-4-piperidinyl)methyl 8-amino-7-chloro-1,4-benzodioxane-5-carboxylate hydrochloride: a highly potent and selective 5-HT4 receptor antagonist derived from metoclopramide. | J Med Chem 36: 4121-3 (1994) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8258836 | 3 | Synthesis and biological evaluation of N4-substituted imidazo- and v-triazolo[4,5-d]pyridazine nucleosides. | J Med Chem 36: 4113-20 (1994) | University of Rhode Island | 2D 3D TSV |
8258834 | 46 | Antipsoriatic anthrones with modulated redox properties. 1. Novel 10-substituted 1,8-dihydroxy-9(10H)-anthracenones as inhibitors of 5-lipoxygenase. | J Med Chem 36: 4099-107 (1994) | Universität Regensburg | 2D 3D TSV |
8258833 | 17 | Synthesis and structure-activity studies of a series of [(hydroxybenzyl)amino]salicylates as inhibitors of EGF receptor-associated tyrosine kinase activity. | J Med Chem 36: 4094-8 (1994) | University of Paris | 2D 3D TSV |
8258832 | 22 | Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB. | J Med Chem 36: 4087-93 (1994) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
8258830 | 87 | Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites. | J Med Chem 36: 4075-81 (1994) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8258829 | 13 | 2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity. | J Med Chem 36: 4069-74 (1993) | University of Urbino | 2D 3D TSV |
8258828 | 15 | Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. 2. 4-(3-Pyridyl)-1(2H)-phthalazinones. | J Med Chem 36: 4061-8 (1994) | Chugai Pharmaceutical Company, Ltd. | 2D 3D TSV |
8258826 | 42 | 6-Substituted benzimidazoles as new nonpeptide angiotensin II receptor antagonists: synthesis, biological activity, and structure-activity relationships. | J Med Chem 36: 4040-51 (1994) | Dr. Karl Thomae GmbH | 2D 3D TSV |
8258825 | 31 | Synthesis of novel modified dipeptide inhibitors of human collagenase: beta-mercapto carboxylic acid derivatives. | J Med Chem 36: 4030-9 (1994) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8258823 | 16 | Xanthines with C8 chiral substituents as potent and selective adenosine A1 antagonists. | J Med Chem 36: 4015-20 (1994) | Marion Merrell Dow Research Institute | 2D 3D TSV |
8258822 | 102 | Three-dimensional quantitative structure-activity relationships of 5-HT receptor binding data for tetrahydropyridinylindole derivatives: a comparison of the Hansch and CoMFA methods. | J Med Chem 36: 4006-14 (1993) | University of Georgia | 2D 3D TSV |
8258821 | 491 | Nanomolar-affinity, non-peptide oxytocin receptor antagonists. | J Med Chem 36: 3993-4005 (1994) | Merck Research Laboratories | 2D 3D TSV |
8258820 | 47 | A novel series of selective, non-peptide inhibitors of angiotensin II binding to the AT2 site. | J Med Chem 36: 3985-92 (1994) | DuPont Pharmaceuticals Company | 2D 3D TSV |
8254628 | 17 | Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists. | J Med Chem 36: 3982-4 (1994) | Eli Lilly and Company | 2D 3D TSV |
8254623 | 54 | Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity. | J Med Chem 36: 3947-55 (1994) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8254620 | 62 | 3,4-Dihydroxychalcones as potent 5-lipoxygenase and cyclooxygenase inhibitors. | J Med Chem 36: 3904-9 (1994) | Tokushima Bunri University | 2D 3D TSV |
8254617 | 20 | R2 C-terminal peptide inhibition of mammalian and yeast ribonucleotide reductase. | J Med Chem 36: 3859-62 (1994) | University of Pennsylvania | 2D 3D TSV |
8254616 | 9 | Novel inhibitors of prolyl 4-hydroxylase. 5. The intriguing structure-activity relationships seen with 2,2'-bipyridine and its 5,5'-dicarboxylic acid derivatives. | J Med Chem 36: 3853-8 (1994) | Zeneca Pharmaceuticals | 2D 3D TSV |
8254615 | 1 | Synthesis of 2,4-disubstituted thiazoles and selenazoles as potential antifilarial and antitumor agents. 2. 2-Arylamido and 2-alkylamido derivatives of 2-amino-4-(isothiocyanatomethyl)thiazole and 2-amino-4-(isothiocyanatomethyl)selenazole. | J Med Chem 36: 3849-52 (1994) | University of Michigan | 2D 3D TSV |
8254612 | 10 | Heterocyclic lactam derivatives as dual angiotensin converting enzyme and neutral endopeptidase 24.11 inhibitors. | J Med Chem 36: 3829-33 (1994) | Ciba-Geigy Corporation | 2D 3D TSV |
8254611 | 12 | Design and synthesis of an orally active macrocyclic neutral endopeptidase 24.11 inhibitor. | J Med Chem 36: 3821-8 (1994) | Ciba-Geigy Corporation | 2D 3D TSV |
8254610 | 14 | Analyses of ligand binding in five endothiapepsin crystal complexes and their use in the design and evaluation of novel renin inhibitors. | J Med Chem 36: 3809-20 (1994) | Warner-Lambert Company | 2D 3D TSV |
8254609 | 61 | Neuropeptide Y: Y1 and Y2 affinities of the complete series of analogues with single D-residue substitutions. | J Med Chem 36: 3802-8 (1994) | Salk Institute | 2D 3D TSV |
8254607 | 36 | Structure-based design of inhibitors of purine nucleoside phosphorylase. 3. 9-Arylmethyl derivatives of 9-deazaguanine substituted on the methylene group. | J Med Chem 36: 3771-83 (1994) | BioCryst Pharmaceuticals Inc | 2D 3D TSV |
8254606 | 55 | Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline. | J Med Chem 36: 3765-70 (1994) | Eisai Co., Ltd | 2D 3D TSV |
8254604 | 50 | Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors. | J Med Chem 36: 3748-56 (1994) | University of Ferrara | 2D 3D TSV |
8254355 | 1 | Isolation and Structure Elucidation of 34-Sulfatobastadin 13, an Inhibitor of the Endothelin A Receptor, from a Marine Sponge of the Genus Ianthella | J Nat Prod 56: 1613-1617 (1993) | TBA | 2D 3D TSV |
8246246 | 13 | A homologous series of permanently charged 1,4-dihydropyridines: novel probes designed to localize drug binding sites on ion channels. | J Med Chem 36: 3743-5 (1994) | State University of New York | 2D 3D TSV |
8246245 | 26 | (Dipropylphenoxy)phenylacetic acids: a new generation of nonpeptide angiotensin II receptor antagonists. | J Med Chem 36: 3738-42 (1994) | Merck Research Laboratories | 2D 3D TSV |
8246244 | 15 | Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists. | J Med Chem 36: 3734-7 (1993) | University of Bologna | 2D 3D TSV |
8246243 | 9 | Photoisomerization of a potent and selective adenosine A2 antagonist, (E)-1,3-Dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine. | J Med Chem 36: 3731-3 (1994) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
8246241 | 34 | 18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography. | J Med Chem 36: 3707-20 (1994) | University of Pennsylvania | 2D 3D TSV |
8246239 | 84 | Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives. | J Med Chem 36: 3693-9 (1994) | Solvay Duphar B.V. | 2D 3D TSV |
8246237 | 30 | HMG-CoA reductase inhibitors: design, synthesis, and biological activity of tetrahydroindazole-substituted 3,5-dihydroxy-6-heptenoic acid sodium salts. | J Med Chem 36: 3674-85 (1994) | R. W. Johnson Pharmaceutical Research Institute | 2D 3D TSV |
8246236 | 6 | Possible contribution of a glutathione conjugate to the long-duration action of beta-funaltrexamine. | J Med Chem 36: 3669-73 (1994) | University of Minnesota | 2D 3D TSV |
8246234 | 13 | Inhibitors of cholesterol biosynthesis. 2. 3,5-Dihydroxy-7-(N-pyrrolyl)-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. | J Med Chem 36: 3658-62 (1994) | Glaxo Group Research Ltd. | 2D 3D TSV |
8246233 | 46 | Inhibitors of cholesterol biosynthesis. 1. 3,5-Dihydroxy-7-(N-imidazolyl)-6-heptenoates and -heptanoates, a novel series of HMG-CoA reductase inhibitors. | J Med Chem 36: 3646-57 (1994) | Glaxo Group Research Ltd. | 2D 3D TSV |
8246229 | 4 | 2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity. | J Med Chem 36: 3611-7 (1994) | Polish Academy of Sciences | 2D 3D TSV |
8246228 | 11 | Transformation of heterocyclic reversible monoamine oxidase-B inactivators into irreversible inactivators by N-methylation. | J Med Chem 36: 3606-10 (1994) | Northwestern University | 2D 3D TSV |
8246227 | 57 | Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates. | J Med Chem 36: 3595-605 (1994) | Merck Research Laboratories | 2D 3D TSV |
8246226 | 89 | Substituted chromenes as potent, orally active 5-lipoxygenase inhibitors. | J Med Chem 36: 3580-94 (1994) | Ciba-Geigy Corporation | 2D 3D TSV |
8246225 | 20 | Analysis of cocaine receptor site ligand binding by three-dimensional Voronoi site modeling approach. | J Med Chem 36: 3572-9 (1994) | University of Michigan | 2D 3D TSV |
8246221 | 90 | The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives. | J Med Chem 36: 3533-41 (1994) | Medical Research Division of American Cyanamid Company | 2D 3D TSV |
8246219 | 16 | Isosteres of the DNA polymerase inhibitor aphidicolin as potential antiviral agents against human herpes viruses. | J Med Chem 36: 3503-10 (1994) | Wellcome Research Laboratories | 2D 3D TSV |
8246171 | 54 | [3H]BIMU-1, a 5-hydroxytryptamine3 receptor ligand in NG-108 cells, selectively labels sigma-2 binding sites in guinea pig hippocampus. | J Pharmacol Exp Ther 267: 961-70 (1993) | Syntex Discovery Research | 2D 3D TSV |
8234299 | 8 | Molecular cloning and characterization of the human A3 adenosine receptor. | Proc Natl Acad Sci U S A 90: 10365-9 (1993) | Merck Research Laboratories | 2D 3D TSV |
8230139 | 165 | Peptide alpha-keto ester, alpha-keto amide, and alpha-keto acid inhibitors of calpains and other cysteine proteases. | J Med Chem 36: 3472-80 (1993) | Georgia Institute of Technology | 2D 3D TSV |
8230138 | 15 | Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some sulfonamidobenzoylglutamate and related derivatives. | J Med Chem 36: 3464-71 (1993) | Wellcome Research Laboratories | 2D 3D TSV |
8230137 | 14 | 9-[(Phosphonoalkyl)benzyl]guanines. Multisubstrate analogue inhibitors of human erythrocyte purine nucleoside phosphorylase. | J Med Chem 36: 3455-63 (1993) | Burroughs Wellcome Co. | 2D 3D TSV |
8230134 | 48 | Synthesis of 5-methyl-5-deaza nonclassical antifolates as inhibitors of dihydrofolate reductases and as potential antipneumocystis, antitoxoplasma, and antitumor agents. | J Med Chem 36: 3437-43 (1993) | Duquesne University | 2D 3D TSV |
8230132 | 7 | New adenosine kinase inhibitors with oral antiinflammatory activity: synthesis and biological evaluation. | J Med Chem 36: 3424-30 (1993) | University of California | 2D 3D TSV |
8230131 | 25 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. | J Med Chem 36: 3409-16 (1993) | Medicinaregatan | 2D 3D TSV |
8230130 | 19 | 3-Nitro-3,4-dihydro-2(1H)-quinolones. Excitatory amino acid antagonists acting at glycine-site NMDA and (RS)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors. | J Med Chem 36: 3397-408 (1993) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
8230127 | 52 | A new series of imidazolones: highly specific and potent nonpeptide AT1 angiotensin II receptor antagonists. | J Med Chem 36: 3371-80 (1993) | Sanofi Recherche | 2D 3D TSV |
8230124 | 92 | Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationships at adenosine receptors. | J Med Chem 36: 3341-9 (1993) | Pharmazeutische Chemie | 2D 3D TSV |
8230123 | 7 | Synthesis and LTB4 receptor antagonist activities of the naturally occurring LTB4 receptor antagonist Leucettamine A and related analogues. | J Med Chem 36: 3333-40 (1993) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8230122 | 32 | Trisubstituted pyridine leukotriene B4 receptor antagonists: synthesis and structure-activity relationships. | J Med Chem 36: 3321-32 (1993) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8230121 | 15 | Synthesis of structural analogs of leukotriene B4 and their receptor binding activity. | J Med Chem 36: 3308-20 (1993) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8230120 | 74 | Inhibitors of acyl-Coa:cholesterol acyltransferase. 4. A novel series of urea ACAT inhibitors as potential hypocholesterolemic agents. | J Med Chem 36: 3300-7 (1993) | Warner-Lambert Company | 2D 3D TSV |
8230117 | 4 | The crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-(3-(cyclopentyloxy)- 4-methoxyphenyl)-pyrrolidin-2-one. | J Med Chem 36: 3274-7 (1993) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8230115 | 16 | Inhibitors of blood platelet cAMP phosphodiesterase. 4. Structural variation of the side-chain terminus of water-soluble 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives. | J Med Chem 36: 3251-64 (1993) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8230109 | 18 | A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor. | J Med Chem 36: 3207-10 (1993) | Merck Research Laboratories | 2D 3D TSV |
8230107 | 61 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. | J Med Chem 36: 3188-96 (1993) | University of Göteborg | 2D 3D TSV |
8230106 | 16 | TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity. | J Med Chem 36: 3182-7 (1993) | Clinical Research Institute of Montreal | 2D 3D TSV |
8230102 | 21 | Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. | J Med Chem 36: 3161-5 (1993) | University of Pennsylvania | 2D 3D TSV |
8230099 | 29 | Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors containing a stereochemically unique peptide isostere. | J Med Chem 36: 3129-36 (1993) | Glaxo Group Research Ltd. | 2D 3D TSV |
8230098 | 46 | A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships. | J Med Chem 36: 3120-8 (1993) | Glaxo Group Research Ltd. | 2D 3D TSV |
8230097 | 7 | A series of penicillin-derived C2-symmetric inhibitors of HIV-1 proteinase: structural and modeling studies. | J Med Chem 36: 3113-9 (1993) | Glaxo Group Research Limited | 2D 3D TSV |
8230096 | 79 | 2,4-Diaminothieno[2,3-d]pyrimidine analogues of trimetrexate and piritrexim as potential inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase. | J Med Chem 36: 3103-12 (1993) | Harvard Medical School | 2D 3D TSV |
8230095 | 11 | Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists. | J Med Chem 36: 3098-102 (1993) | Sandoz Research Institute | 2D 3D TSV |
8230093 | 34 | Conformationally restrained analogs of sympathomimetic catecholamines. Synthesis, conformational analysis, and adrenergic activity of isochroman derivatives. | J Med Chem 36: 3077-86 (1993) | Universit£ di Pisa | 2D 3D TSV |
8226867 | 41 | Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. | J Biol Chem 268: 23422-6 (1993) | Synaptic Pharmaceutical Corporation | 2D 3D TSV |
8224165 | 18 | Cloning and characterization of the rat 5-HT5B receptor. Evidence that the 5-HT5B receptor couples to a G protein in mammalian cell membranes. | FEBS Lett 333: 25-31 (1993) | University of Heidelberg ZMBH | 2D 3D TSV |
8201608 | 28 | Molecular similarity, quantitative chirality, and QSAR for chiral drugs. | J Med Chem 37: 1727-32 (1994) | University of Oxford | 2D 3D TSV |
8201607 | 50 | 2-Alkynyl derivatives of adenosine-5'-N-ethyluronamide: selective A2 adenosine receptor agonists with potent inhibitory activity on platelet aggregation. | J Med Chem 37: 1720-6 (1994) | Universit£ di Camerino | 2D 3D TSV |
8201606 | 2 | Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 2. 2-Phenoxy-, 2-(phenylthio)-, and 2-(phenylamino)alkanoic acid esters. | J Med Chem 37: 1712-9 (1994) | Universit£ di Firenze | 2D 3D TSV |
8201605 | 3 | Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 1. Tropic and 2-phenylpropionic acid esters. | J Med Chem 37: 1704-11 (1994) | Universit£ di Firenze | 2D 3D TSV |
8201604 | 96 | Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues. | J Med Chem 37: 1696-703 (1994) | Rhône-Poulenc Rorer | 2D 3D TSV |
8201603 | 5 | Structural studies on bioactive compounds. 23. Synthesis of polyhydroxylated 2-phenylbenzothiazoles and a comparison of their cytotoxicities and pharmacological properties with genistein and quercetin. | J Med Chem 37: 1689-95 (1994) | University of Nottingham | 2D 3D TSV |
8201600 | 41 | Antipsoriatic anthrones with modulated redox properties. 2. Novel derivatives of chrysarobin and isochrysarobin--antiproliferative activity and 5-lipoxygenase inhibition. | J Med Chem 37: 1660-9 (1994) | Universität Regensburg | 2D 3D TSV |
8201599 | 51 | Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). 7. Development of a series of substituted N-phenyl-N'-[(1-phenylcyclopentyl)methyl]ureas with enhanced hypocholesterolemic activity. | J Med Chem 37: 1652-9 (1994) | Warner-Lambert Company | 2D 3D TSV |
8201598 | 15 | Synthesis and carbonic anhydrase inhibitory activity of 4-substituted 2-thiophenesulfonamides. | J Med Chem 37: 1646-51 (1994) | Allergan Inc | 2D 3D TSV |
8201597 | 10 | Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives. | J Med Chem 37: 1632-45 (1994) | E. Merck | 2D 3D TSV |
8201595 | 12 | Synthesis and antitumor activities of novel 6-5 fused ring heterocycle antifolates: N-[4-[omega-(2-amino-4-substituted-6,7-dihydrocyclopenta [d]pyrimidin-5-yl)alkyl]benzoyl]-L-glutamic acids. | J Med Chem 37: 1616-24 (1994) | Eisai Company, Ltd | 2D 3D TSV |
8201592 | 27 | [L-Ala3]DPDPE: a new enkephalin analog with a unique opioid receptor activity profile. Further evidence of delta-opioid receptor multiplicity. | J Med Chem 37: 1572-7 (1994) | University of Arizona | 2D 3D TSV |
8201591 | 2 | CCK-A-selective tetrapeptides containing lys(N epsilon)-amide residues: favorable in vivo and in vitro effects of N-methylation at the aspartyl residue. | J Med Chem 37: 1569-71 (1994) | Abbott Laboratories | 2D 3D TSV |
8201590 | 20 | Novel Asp32-replacement tetrapeptide analogues as potent and selective CCK-A agonists. | J Med Chem 37: 1562-8 (1994) | Abbott Laboratories | 2D 3D TSV |
8201589 | 11 | N-omega-fluoroalkyl analogs of (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)-tropane (beta-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters. | J Med Chem 37: 1558-61 (1994) | Research Biochemicals International | 2D 3D TSV |
8201588 | 14 | 1,3-Diarylindan-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists. | J Med Chem 37: 1553-7 (1994) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8201586 | 3 | 2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]acetamide: an opioid receptor affinity label that produces selective and long-lasting kappa antagonism in mice. | J Med Chem 37: 1547-9 (1994) | University of Minnesota | 2D 3D TSV |
8190112 | 3 | 125I-4-aminobenzyl-5'-N-methylcarboxamidoadenosine, a high affinity radioligand for the rat A3 adenosine receptor. | Mol Pharmacol 45: 978-82 (1994) | Duke University | 2D 3D TSV |
8182712 | 14 | Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents. | J Med Chem 37: 1535-42 (1994) | University of Tennessee at Knoxville | 2D 3D TSV |
8182711 | 39 | Synthesis and structure-activity relationships of deazaxanthines: analogs of potent A1- and A2-adenosine receptor antagonists. | J Med Chem 37: 1526-34 (1994) | Eberhard-Karls-Universität Tübingen | 2D 3D TSV |
8182708 | 18 | Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor. | J Med Chem 37: 1495-500 (1994) | University of Minnesota | 2D 3D TSV |
8182702 | 14 | Search for the pharmacophore of bispyridinium-type allosteric modulators of muscarinic receptors. | J Med Chem 37: 1439-45 (1994) | University of Bonn | 2D 3D TSV |
8182701 | 39 | Novel ligands specific for mitochondrial benzodiazepine receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives. Synthesis, structure-activity relationships, and molecular modeling studies. | J Med Chem 37: 1427-38 (1994) | Universit£ di Siena | 2D 3D TSV |
8182697 | 11 | Synthesis and evaluation of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p- iodobenzamido]ethyl]piperazine (p-MPPI): a new iodinated 5-HT1A ligand. | J Med Chem 37: 1406-7 (1994) | University of Pennsylvania | 2D 3D TSV |
8182696 | 10 | 3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor. | J Med Chem 37: 1402-5 (1994) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
8176711 | 18 | Protein kinase C. Modeling of the binding site and prediction of binding constants. | J Med Chem 37: 1326-38 (1994) | National Cancer Institute-Bethesda | 2D 3D TSV |
8176710 | 24 | Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties. | J Med Chem 37: 1320-5 (1994) | CIFA Universidad de Navarra | 2D 3D TSV |
8176709 | 32 | 6-Alkyl- and 6-arylandrost-4-ene-3,17-diones as aromatase inhibitors. Synthesis and structure-activity relationships. | J Med Chem 37: 1312-9 (1994) | Tohoku College of Pharmacy | 2D 3D TSV |
8176706 | 27 | Synthesis, structure-activity relationships, and pharmacological evaluation of a series of fluorinated 3-benzyl-5-indolecarboxamides: identification of 4-[[5-[((2R)-2-methyl-4,4,4-trifluorobutyl)carbamoyl]-1-methyl indol- 3-yl]methyl]-3-methoxy-N-[(2-methylphenyl)sulfonyl]benzamide, a potent, orall | J Med Chem 37: 1282-97 (1994) | Zeneca Pharmaceuticals Group | 2D 3D TSV |
8176705 | 25 | Aromatase inhibitors. Syntheses and structure-activity studies of novel pyridyl-substituted indanones, indans, and tetralins. | J Med Chem 37: 1275-81 (1994) | Universität des Saarlandes | 2D 3D TSV |
8176704 | 40 | Synthesis of 2 beta-acyl-3 beta-aryl-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites in rat striatum and frontal cortex. | J Med Chem 37: 1262-8 (1994) | Wake Forest University | 2D 3D TSV |
8176703 | 14 | Design of orally active, non-peptidic inhibitors of human leukocyte elastase. | J Med Chem 37: 1259-61 (1994) | Zeneca Pharmaceuticals Group | 2D 3D TSV |
8176701 | 4 | Potent, selective, and systemically-available inhibitors of acyl-coenzyme A:cholesterol acyl transferase (ACAT). | J Med Chem 37: 1252-5 (1994) | Pfizer Inc | 2D 3D TSV |
8176700 | 1 | Applications of combinatorial technologies to drug discovery. 1. Background and peptide combinatorial libraries. | J Med Chem 37: 1233-51 (1994) | Affymax Research Institute | 2D 3D TSV |
8176401 | 21 | Anti-AIDS Agents, 11. Betulinic Acid and Platanic Acid as Anti-HIV Principles from Syzigium claviflorum, and the Anti-HIV Activity of Structurally Related Triterpenoids | J Nat Prod 57: 243-247 (1994) | TBA | 2D 3D TSV |
8171040 | 10 | L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor. | Proc Natl Acad Sci U S A 91: 4096-100 (1994) | Merck Research Laboratories | 2D 3D TSV |
8169832 | 9 | Characterization of a 5-hydroxytryptamine receptor in mouse neuroblastoma N18TG2 cells. | J Pharmacol Exp Ther 269: 246-55 (1994) | University of Pennsylvania | 2D 3D TSV |
8164265 | 42 | Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters. | J Med Chem 37: 1220-3 (1994) | National Institute on Drug Abuse | 2D 3D TSV |
8164264 | 56 | Structural features important for sigma 1 receptor binding. | J Med Chem 37: 1214-9 (1994) | Virginia Commonwealth University | 2D 3D TSV |
8164262 | 38 | Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors. | J Med Chem 37: 1200-7 (1994) | Daiichi Pharmaceutical Company, Ltd. | 2D 3D TSV |
8164260 | 23 | The development of cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors. | J Med Chem 37: 1177-88 (1994) | Merck Research Laboratories | 2D 3D TSV |
8164259 | 44 | Classical and nonclassical furo[2,3-d]pyrimidines as novel antifolates: synthesis and biological activities. | J Med Chem 37: 1169-76 (1994) | Duquesne University | 2D 3D TSV |
8164257 | 18 | Thiopyrano[2,3,4-cd]indoles as 5-lipoxygenase inhibitors: synthesis, biological profile, and resolution of 2-[2-[1-(4-chlorobenzyl)-4-methyl-6-[(5-phenylpyridin-2-yl)methoxy]-4,5 -dihydro-1H-thiopyrano[2,3,4-cd]indol-2-yl]ethoxy]butanoic acid. | J Med Chem 37: 1153-64 (1994) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
8164256 | 6 | Calculation of relative differences in the binding free energies of HIV1 protease inhibitors: a thermodynamic cycle perturbation approach. | J Med Chem 37: 1145-52 (1994) | Agouron Pharmaceuticals Inc | 2D 3D TSV |
8164255 | 23 | Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects. | J Med Chem 37: 1136-44 (1994) | Clinical Research Institute of Montreal | 2D 3D TSV |
8164254 | 48 | Antitumor agents. 150. 2',3',4',5',5,6,7-substituted 2-phenyl-4-quinolones and related compounds: their synthesis, cytotoxicity, and inhibition of tubulin polymerization. | J Med Chem 37: 1126-35 (1994) | School of Pharmacy | 2D 3D TSV |
8164252 | 18 | Structure-based design of inhibitors of purine nucleoside phosphorylase. 4. A study of phosphate mimics. | J Med Chem 37: 1109-14 (1994) | Ciba-Geigy Corporation | 2D 3D TSV |
8164250 | 54 | New dual inhibitors of neutral endopeptidase and angiotensin-converting enzyme: rational design, bioavailability, and pharmacological responses in experimental hypertension. | J Med Chem 37: 1070-83 (1994) | University of Paris | 2D 3D TSV |
8164249 | 46 | Application of the three-dimensional structures of protein target molecules in structure-based drug design. | J Med Chem 37: 1035-54 (1994) | Abbott Laboratories | 2D 3D TSV |
8161940 | 9 | Melatonin receptors: localization, molecular pharmacology and physiological significance. | Neurochem Int 24: 101-46 (1994) | Rowett Research Institute | 2D 3D TSV |
8158166 | 2 | Isolation of bioactive and other oxoaporphine alkaloids from two annonaceous plants, Xylopia aethiopica and Miliusa cf. banacea. | J Nat Prod 57: 68-73 (1994) | Virginia Polytechnic Institute and State University | 2D 3D TSV |
8158162 | 2 | Verongamine, a Novel Bromotyrosine-Derived Histamine H3-Antagonist from the Marine Sponge Verongula gigantea | J Nat Prod 57: 175-177 (1994) | TBA | 2D 3D TSV |
8155646 | 3 | Selective activation of inhibitory G-protein alpha-subunits by partial agonists of the human 5-HT1A receptor. | Biochemistry 33: 4283-90 (1994) | Medical University of South Carolina | 2D 3D TSV |
8151626 | 4 | Antiinflammatory 4,5-diarylpyrroles: synthesis and QSAR. | J Med Chem 37: 988-98 (1994) | DuPont Pharmaceuticals Company | 2D 3D TSV |
8151622 | 22 | Development of a receptor-interaction model for serotonin 5-HT2 receptor antagonists. Predicting selectivity with respect to dopamine D2 receptors. | J Med Chem 37: 950-62 (1994) | H. Lundbeck A/S | 2D 3D TSV |
8151612 | 88 | Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase. | J Med Chem 37: 1015-27 (1994) | Ciba-Geigy Limited | 2D 3D TSV |
8145238 | 4 | The novel Ins(1,4,5)P3 analogue 3-amino-3-deoxy-Ins(1,4,5)P3: a pH-dependent Ins(1,4,5)P3 receptor partial agonist in SH-SY5Y neuroblastoma cells. | J Med Chem 37: 868-72 (1994) | Mayo Foundation | 2D 3D TSV |
8145236 | 86 | Structure-activity relationships in a series of 5-[(2,5-dihydroxybenzyl)amino]salicylate inhibitors of EGF-receptor-associated tyrosine kinase: importance of additional hydrophobic aromatic interactions. | J Med Chem 37: 845-59 (1994) | University of Paris | 2D 3D TSV |
8145235 | 9 | Benzo[f]quinazoline inhibitors of thymidylate synthase: methyleneamino-linked aroylglutamate derivatives. | J Med Chem 37: 838-44 (1994) | Wellcome Research Laboratories | 2D 3D TSV |
8145231 | 47 | Inhibitors of acyl-CoA:cholesterol acyltransferase. 1. Synthesis and hypocholesterolemic activity of dibenz[b,e]oxepin-11-carboxanilides. | J Med Chem 37: 804-10 (1994) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
8145228 | 15 | Molecular modeling studies of aldose reductase inhibitors. | J Med Chem 37: 787-92 (1994) | National Eye Institute | 2D 3D TSV |
8145226 | 45 | Conformationally constrained peptides and semipeptides derived from RGD as potent inhibitors of the platelet fibrinogen receptor and platelet aggregation. | J Med Chem 37: 769-80 (1994) | SmithKline Beecham Pharmaceuticals Research and Development | 2D 3D TSV |
8145225 | 2 | Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. | J Med Chem 37: 758-68 (1994) | Upjohn Laboratories | 2D 3D TSV |
8145221 | 28 | Pseudopeptide inhibitors of Ras farnesyl-protein transferase. | J Med Chem 37: 725-32 (1994) | Merck Research Laboratories | 2D 3D TSV |
8145220 | 16 | Second-generation benzodiazepine CCK-B antagonists. Development of subnanomolar analogs with selectivity and water solubility. | J Med Chem 37: 722-4 (1994) | Merck Research Laboratories | 2D 3D TSV |
8145219 | 20 | High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group. | J Med Chem 37: 719-21 (1994) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
8145218 | 8 | 3-Alkoxybenzo[b]thiophene-2-carboxamides as inhibitors of neutrophil-endothelial cell adhesion. | J Med Chem 37: 717-8 (1994) | Warner-Lambert Company | 2D 3D TSV |
8126709 | 49 | Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity. | J Med Chem 37: 689-95 (1994) | Centre de Recherche Pierre Fabre Médicament | 2D 3D TSV |
8126708 | 113 | Matrix metalloproteinase inhibitors containing a (carboxyalkyl)amino zinc ligand: modification of the P1 and P2' residues. | J Med Chem 37: 674-88 (1994) | Glaxo Inc. Research Institute | 2D 3D TSV |
8126707 | 18 | Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases. | J Med Chem 37: 665-73 (1994) | University of California | 2D 3D TSV |
8126705 | 8 | Modulation of the kynurenine pathway in search for new neuroprotective agents. Synthesis and preliminary evaluation of (m-nitrobenzoyl)alanine, a potent inhibitor of kynurenine-3-hydroxylase. | J Med Chem 37: 647-55 (1994) | Universit£ di Perugia | 2D 3D TSV |
8126704 | 79 | Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists. | J Med Chem 37: 636-46 (1994) | National Institute of Diabetes | 2D 3D TSV |
8126703 | 29 | Tetrapeptide CCK-A agonists: effect of backbone N-methylations on in vitro and in vivo CCK activity. | J Med Chem 37: 630-5 (1994) | Abbott Laboratories | 2D 3D TSV |
8126701 | 3 | Molecular modeling studies on ligand binding to sialidase from influenza virus and the mechanism of catalysis. | J Med Chem 37: 616-24 (1994) | Monash University | 2D 3D TSV |
8126697 | 30 | Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety. | J Med Chem 37: 579-85 (1994) | University of Minnesota | 2D 3D TSV |
8126695 | 35 | 1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor. | J Med Chem 37: 565-71 (1994) | Merck Research Laboratories | 2D 3D TSV |
8126693 | 2 | Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity. | J Med Chem 37: 560-2 (1994) | Warner-Lambert Company | 2D 3D TSV |
8126692 | 31 | Discovery of new non-phospholipid inhibitors of the secretory phospholipases A2. | J Med Chem 37: 557-9 (1994) | Fisons plc | 2D 3D TSV |
8120872 | 2 | Antiviral enantiomeric preference for 5'-noraristeromycin. | J Med Chem 37: 551-4 (1994) | University of South Florida | 2D 3D TSV |
8120871 | 19 | Pyrido[2,3-d]pyrimidine angiotensin II antagonists. | J Med Chem 37: 542-50 (1994) | Wyeth-Ayerst Research | 2D 3D TSV |
8120869 | 10 | Naphthalenic lignan lactones as selective, nonredox 5-lipoxygenase inhibitors. Synthesis and biological activity of (methoxyalkyl)thiazole and methoxytetrahydropyran hybrids. | J Med Chem 37: 512-8 (1994) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
8120868 | 22 | N-Phosphonomethyl dipeptides and their phosphonate prodrugs, a new generation of neutral endopeptidase (NEP, EC 3.4.24.11) inhibitors. | J Med Chem 37: 498-511 (1994) | Ciba-Geigy Corporation | 2D 3D TSV |
8120867 | 70 | Non-peptide renin inhibitors containing 2-(((3-phenylpropyl)phosphoryl)oxy)alkanoic acid moieties as P2-P3 replacements. | J Med Chem 37: 486-97 (1994) | E. Merck Darmstadt | 2D 3D TSV |
8120866 | 54 | Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine. | J Med Chem 37: 476-85 (1994) | SmithKline Beecham Pharmaceuticals Ltd | 2D 3D TSV |
8120863 | 47 | Potent gastrin-releasing peptide (GRP) antagonists derived from GRP (19-27) with a C-terminal DPro psi [CH2NH]Phe-NH2 and N-terminal aromatic residues. | J Med Chem 37: 439-45 (1994) | Burroughs Wellcome Company | 2D 3D TSV |
8114680 | 110 | Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors. | Mol Pharmacol 45: 330-4 (1994) | University of Pennsylvania | 2D 3D TSV |
8105084 | 6 | Non-amine based analogues of lavendustin A as protein-tyrosine kinase inhibitors. | J Med Chem 36: 3010-4 (1993) | National Institutes of Health | 2D 3D TSV |
8102973 | 31 | Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications. | Eur J Pharmacol 236: 483-6 (1993) | Maryland Psychiatric Research Center | 2D 3D TSV |
8102785 | 91 | Characterization of cloned somatostatin receptors SSTR4 and SSTR5. | Mol Pharmacol 44: 385-92 (1993) | University of Pennsylvania | 2D 3D TSV |
8102651 | 53 | Synthesis and pharmacological evaluation of 1-phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes as ligands for a novel receptor with sigma-like neuromodulatory activity. | J Med Chem 36: 2542-51 (1993) | University of North Carolina | 2D 3D TSV |
8101878 | 61 | Studies on quinazolines. 5. 2,3-dihydroimidazo[1,2-c]quinazoline derivatives: a novel class of potent and selective alpha 1-adrenoceptor antagonists and antihypertensive agents. | J Med Chem 36: 2196-207 (1993) | National Defense Medical Center | 2D 3D TSV |
8101877 | 80 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. | J Med Chem 36: 2107-14 (1993) | University of Liège | 2D 3D TSV |
8101876 | 28 | Novel 2-substituted tetrahydro-3H-benz[e]indolamines: highly potent and selective agonists acting at the 5-HT1A receptor as possible anxiolytics and antidepressants. | J Med Chem 36: 2066-74 (1993) | Upjohn Laboratories | 2D 3D TSV |
8100352 | 4 | Cloning and expression of a human somatostatin-14-selective receptor variant (somatostatin receptor 4) located on chromosome 20. | Mol Pharmacol 43: 894-901 (1993) | University of Toronto | 2D 3D TSV |
8100350 | 137 | Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides. | Mol Pharmacol 43: 838-44 (1993) | University of Pennsylvania | 2D 3D TSV |
8100134 | 109 | Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics. | Biochem Pharmacol 45: 2352-4 (1993) | Mayo Foundation | 2D 3D TSV |
8099976 | 3 | Synthesis of isosteric analogues of nicotinamide adenine dinucleotide containing C-nucleotide of nicotinamide or picolinamide. | J Med Chem 36: 1855-9 (1993) | Cornell University | 2D 3D TSV |
8099194 | 2 | Unique binding characteristics of antipsychotic agents interacting with human dopamine D2A, D2B, and D3 receptors. | Mol Pharmacol 43: 749-54 (1993) | Astra Arcus AB | 2D 3D TSV |
8098771 | 19 | Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand. | J Med Chem 36: 1499-500 (1993) | University of Pennsylvania | 2D 3D TSV |
8098066 | 39 | Synthesis and biological evaluation of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine homologues at dopamine-uptake and phencyclidine- and sigma-binding sites. | J Med Chem 36: 1188-93 (1993) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8097539 | 10 | Synthesis and opioid activity of dynorphin A-(1-13)NH2 analogues containing cis- and trans-4-aminocyclohexanecarboxylic acid. | J Med Chem 36: 1100-3 (1993) | Oregon State University | 2D 3D TSV |
8097538 | 69 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. | J Med Chem 36: 1069-83 (1993) | Upjohn Laboratories | 2D 3D TSV |
8097537 | 91 | Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives. | J Med Chem 36: 1053-68 (1993) | Upjohn Laboratories | 2D 3D TSV |
8097479 | 3 | A human somatostatin receptor (SSTR3), located on chromosome 22, displays preferential affinity for somatostatin-14 like peptides. | FEBS Lett 321: 279-84 (1993) | University of Toronto | 2D 3D TSV |
8097160 | 35 | Dopamine D4 receptors bind inactive (+)-aporphines, suggesting neuroleptic role. Sulpiride not stereoselective. | Eur J Pharmacol 233: 173-4 (1993) | University of Toronto | 2D 3D TSV |
8096548 | 27 | Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system. | J Med Chem 36: 912-8 (1993) | Eli Lilly and Company | 2D 3D TSV |
8096246 | 70 | Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs. | J Med Chem 36: 750-7 (1993) | University of Arizona | 2D 3D TSV |
8093908 | 15 | Dibenz[b,e]oxepin derivatives: novel antiallergic agents possessing thromboxane A2 and histamine H1 dual antagonizing activity. 1. | J Med Chem 36: 417-20 (1993) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
8093734 | 11 | Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT. | J Med Chem 36: 221-8 (1993) | University of Pennsylvania | 2D 3D TSV |
8093723 | 20 | Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties. | J Pharmacol Exp Ther 264: 158-65 (1993) | Dainippon Pharmaceutical Co., Ltd | 2D 3D TSV |
8093626 | 13 | o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents. | J Med Chem 36: 157-61 (1993) | Università di Perugia | 2D 3D TSV |
8078486 | 15 | Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor. | Mol Pharmacol 46: 227-34 (1994) | Eli Lilly and Company | 2D 3D TSV |
8071944 | 37 | 8-Azaxanthine derivatives as antagonists of adenosine receptors. | J Med Chem 37: 2970-5 (1994) | Università di Camerino | 2D 3D TSV |
8071941 | 240 | Synthesis and structure-activity relationships of novel retinoid X receptor-selective retinoids. | J Med Chem 37: 2930-41 (1994) | Ligand Pharmaceuticals Inc | 2D 3D TSV |
8071940 | 32 | Stereospecific synthesis of peptidyl alpha-keto amides as inhibitors of calpain. | J Med Chem 37: 2918-29 (1994) | Alkermes, Inc. | 2D 3D TSV |
8071935 | 25 | Synthesis, ligand binding, and QSAR (CoMFA and classical) study of 3 beta-(3'-substituted phenyl)-, 3 beta-(4'-substituted phenyl)-, and 3 beta-(3',4'-disubstituted phenyl)tropane-2 beta-carboxylic acid methyl esters. | J Med Chem 37: 2865-73 (1994) | Research Triangle Institute | 2D 3D TSV |
8071934 | 30 | Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide. | J Med Chem 37: 2856-64 (1994) | University of Washington | 2D 3D TSV |
8071931 | 20 | 5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist. | J Med Chem 37: 2828-30 (1994) | Medical College of Virginia/Virginia Commonwealth University | 2D 3D TSV |
8064808 | 202 | Triazolinone biphenylsulfonamide derivatives as orally active angiotensin II antagonists with potent AT1 receptor affinity and enhanced AT2 affinity. | J Med Chem 37: 2808-24 (1994) | Merck Research Laboratories | 2D 3D TSV |
8064804 | 3 | Design, synthesis, and neurochemical evaluation of 2-amino-5-(alkoxycarbonyl)-3,4,5,6-tetrahydropyridines and 2-amino-5-(alkoxycarbonyl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists. | J Med Chem 37: 2774-82 (1994) | University of Toledo | 2D 3D TSV |
8064803 | 43 | Structure-affinity relationship studies on 5-HT1A receptor ligands. 2. Heterobicyclic phenylpiperazines with N4-aralkyl substituents. | J Med Chem 37: 2761-73 (1994) | Solvay Duphar Research Laboratories | 2D 3D TSV |
8064802 | 9 | Structure-activity relationship studies of central nervous system agents. 13. 4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a new putative 5-HT1A receptor antagonist, and its analogs. | J Med Chem 37: 2754-60 (1994) | Polish Academy of Sciences | 2D 3D TSV |
8064801 | 232 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. | J Med Chem 37: 2735-53 (1994) | University of G£teborg | 2D 3D TSV |
8064800 | 32 | Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase. | J Med Chem 37: 2721-34 (1994) | Pfizer Inc | 2D 3D TSV |
8064799 | 16 | Cyclic peptides with a phosphinic bond as potent inhibitors of a zinc bacterial collagenase. | J Med Chem 37: 2713-20 (1994) | University of Athens | 2D 3D TSV |
8064798 | 44 | Substituted 1,3-dipropylxanthines as irreversible antagonists of A1 adenosine receptors. | J Med Chem 37: 2704-12 (1994) | University of South Florida | 2D 3D TSV |
8064797 | 118 | Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. | J Med Chem 37: 2686-96 (1994) | Vanderbilt University | 2D 3D TSV |
8064796 | 10 | Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substituted)glycine peptoid library. | J Med Chem 37: 2678-85 (1994) | Chiron Corporation | 2D 3D TSV |
8064795 | 29 | A novel nonpeptide HIV-1 protease inhibitor: elucidation of the binding mode and its application in the design of related analogs. | J Med Chem 37: 2664-77 (1994) | Parke-Davis Pharmaceutical Research | 2D 3D TSV |
8064792 | 25 | 5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase. | J Med Chem 37: 2627-9 (1994) | Sterling Winthrop Pharmaceuticals Research Division | 2D 3D TSV |
8064791 | 18 | 2,6-Disubstituted aryl carboxylic acids, leaving groups"par excellence" for benzisothiazolone inhibitors of human leukocyte elastase. | J Med Chem 37: 2623-6 (1994) | Sterling Winthrop Pharmaceutical Research Division | 2D 3D TSV |
8064298 | 9 | SB-202742, a novel beta-lactamase inhibitor isolated from Spondias mombin. | J Nat Prod 57: 654-7 (1994) | SmithKline Beecham Pharmaceuticals | 2D 3D TSV |
8057300 | 28 | Spirovesamicols: conformationally restricted analogs of 2-(4-phenylpiperidino)cyclohexanol (vesamicol, AH5183) as potential modulators of presynaptic cholinergic function. | J Med Chem 37: 2574-82 (1994) | University of Minnesota | 2D 3D TSV |
8057299 | 66 | Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp. | J Med Chem 37: 2537-51 (1994) | Merck Research Laboratories | 2D 3D TSV |
8057297 | 24 | 5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity. | J Med Chem 37: 2509-12 (1994) | Pfizer Inc | 2D 3D TSV |
8057296 | 4 | Structure-based design of HIV-1 protease inhibitors: replacement of two amides and a 10 pi-aromatic system by a fused bis-tetrahydrofuran. | J Med Chem 37: 2506-8 (1994) | Merck Research Laboratories | 2D 3D TSV |
8057293 | 25 | Structure-based design of inhibitors of purine nucleoside phosphorylase. 5. 9-Deazahypoxanthines. | J Med Chem 37: 2477-80 (1994) | Southern Research Institute | 2D 3D TSV |
8057292 | 83 | Mercaptoacyl amino acid inhibitors of atriopeptidase. 1. Structure-activity relationship studies of methionine and S-alkylcysteine derivatives. | J Med Chem 37: 2461-76 (1994) | Schering-Plough Research Institute | 2D 3D TSV |
8057289 | 17 | Leukotriene B4 (LTB4) receptor antagonists: a series of (hydroxyphenyl)pyrazoles. | J Med Chem 37: 2411-20 (1994) | Eli Lilly and Company | 2D 3D TSV |
8057287 | 77 | Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 11. Structure-activity relationships of several series of compounds derived from N-(chlorocarbonyl) isocyanate. | J Med Chem 37: 2394-400 (1994) | Warner-Lambert Company | 2D 3D TSV |
8057285 | 44 | Synthesis and SAR studies of novel triazolopyrimidine derivatives as potent, orally active angiotensin II receptor antagonists. | J Med Chem 37: 2371-86 (1994) | Carpibem | 2D 3D TSV |
8057283 | 126 | 6-Azasteroids: 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. | J Med Chem 37: 2352-60 (1994) | Glaxo Inc. Research Institute | 2D 3D TSV |
8057282 | 2 | Design and synthesis of seco-oxysterol analogs as potential inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase gene transcription. | J Med Chem 37: 2343-51 (1994) | Upjohn Laboratories | 2D 3D TSV |
8057281 | 100 | Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. | J Med Chem 37: 2334-42 (1994) | Synaptic Pharmaceutical Corporation | 2D 3D TSV |
8057278 | 43 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. | J Med Chem 37: 2292-9 (1994) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
8057277 | 54 | Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands. | J Med Chem 37: 2285-91 (1994) | National Institute on Drug Abuse-Intramural Research Program | 2D 3D TSV |
8057276 | 11 | Crystal-structure-based design and synthesis of novel C-terminal inhibitors of HIV protease. | J Med Chem 37: 2274-84 (1994) | Agouron Pharmaceuticals Inc | 2D 3D TSV |
8057274 | 18 | Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders. | J Med Chem 37: 2262-5 (1994) | Eli Lilly and Company | 2D 3D TSV |
8057273 | 9 | Novel 3 alpha-(diphenylmethoxy)tropane analogs: potent dopamine uptake inhibitors without cocaine-like behavioral profiles. | J Med Chem 37: 2258-61 (1994) | National Institutes of Health | 2D 3D TSV |
8057272 | 33 | Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists. | J Med Chem 37: 2253-7 (1994) | Glaxo Research and Development Ltd. | 2D 3D TSV |
8035432 | 5 | Synthesis of substituted 3-carbamoylecgonine methyl ester analogues: irreversible and photoaffinity ligands for the cocaine receptor/dopamine transporter. | J Med Chem 37: 2249-52 (1994) | University of Maryland | 2D 3D TSV |
8035428 | 30 | Three-dimensional quantitative structure-activity relationship of human immunodeficiency virus (I) protease inhibitors. 2. Predictive power using limited exploration of alternate binding modes. | J Med Chem 37: 2206-15 (1994) | Washington University | 2D 3D TSV |
8035427 | 51 | Synthesis of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their related 7-deoxy analogs as conformational and catalytic probes for the active site of aromatase. | J Med Chem 37: 2198-205 (1994) | Tohoku College of Pharmacy | 2D 3D TSV |
8035423 | 12 | Synthesis and biological activity of N omega-hemiphthaloyl-alpha,omega- diaminoalkanoic acid analogues of aminopterin and 3',5-dichloroaminopterin. | J Med Chem 37: 2167-74 (1994) | Harvard Medical School | 2D 3D TSV |
8035422 | 17 | S-(N-aryl-N-hydroxycarbamoyl)glutathione derivatives are tight-binding inhibitors of glyoxalase I and slow substrates for glyoxalase II. | J Med Chem 37: 2161-6 (1994) | University of Maryland | 2D 3D TSV |
8035420 | 13 | 4-[(Alkylamino)methyl]furo[3,2-c]pyridines: a new series of selective kappa-receptor agonists. | J Med Chem 37: 2138-44 (1994) | Glaxo Group Research Ltd. | 2D 3D TSV |
8035419 | 122 | A new series of PDGF receptor tyrosine kinase inhibitors: 3-substituted quinoline derivatives. | J Med Chem 37: 2129-37 (1994) | Rhône-Poulenc Rorer | 2D 3D TSV |
8035418 | 30 | Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist. | J Med Chem 37: 2125-8 (1994) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
8035417 | 23 | Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling. | J Med Chem 37: 2122-4 (1994) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
8035312 | 23 | Ligand specificity of nicotinic acetylcholine receptors in rat spinal cord: studies with nicotine and cytisine. | J Pharmacol Exp Ther 270: 159-66 (1994) | University of California | 2D 3D TSV |
8027993 | 4 | Thienyl and thiazolyl acyclic analogues of 5-deazatetrahydrofolic acid. | J Med Chem 37: 2112-5 (1994) | Wellcome Research Laboratories | 2D 3D TSV |
8027992 | 49 | Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity. | J Med Chem 37: 2106-11 (1994) | Eisai Company, Ltd | 2D 3D TSV |
8027991 | 26 | Identification of two hydrophobic patches in the active-site cavity of human carbonic anhydrase II by solution-phase and solid-state studies and their use in the development of tight-binding inhibitors. | J Med Chem 37: 2100-5 (1994) | Harvard University | 2D 3D TSV |
8027990 | 25 | Selective inhibitors of monoamine oxidase. 2. Arylamide SAR. | J Med Chem 37: 2085-9 (1994) | Burroughs Wellcome Company | 2D 3D TSV |
8027989 | 28 | Novel acyl-CoA:cholesterol acyltransferase inhibitors. Synthesis and biological activity of 3-quinolylurea derivatives. | J Med Chem 37: 2079-84 (1994) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
8027988 | 37 | New potent prolyl endopeptidase inhibitors: synthesis and structure-activity relationships of indan and tetralin derivatives and their analogues. | J Med Chem 37: 2071-8 (1994) | Zeria Pharmaceutical Company, Ltd. | 2D 3D TSV |
8027987 | 1 | N-substituted spirosuccinimide, spiropyridazine, spiroazetidine, and acetic acid aldose reductase inhibitors derived from isoquinoline-1,3-diones. 2. | J Med Chem 37: 2059-70 (1994) | Wyeth-Ayerst Research Inc. | 2D 3D TSV |
8027986 | 30 | Novel spirosuccinimide aldose reductase inhibitors derived from isoquinoline-1,3-diones: 2-[(4-bromo-2-fluorophenyl)methyl]-6- fluorospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrone and congeners. 1. | J Med Chem 37: 2043-58 (1994) | Wyeth-Ayerst Research | 2D 3D TSV |
8027985 | 66 | Tyrosine kinase inhibitors. 3. Structure-activity relationships for inhibition of protein tyrosine kinases by nuclear-substituted derivatives of 2,2'-dithiobis(1-methyl-N-phenyl-1H-indole-3-carboxamide). | J Med Chem 37: 2033-42 (1994) | University of Auckland | 2D 3D TSV |
8027984 | 93 | 3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a novel series of platelet activating factor antagonists. | J Med Chem 37: 2011-32 (1994) | Abbott Laboratories | 2D 3D TSV |
8027983 | 16 | The discovery of an unusually selective and novel cocaine analog: difluoropine. Synthesis and inhibition of binding at cocaine recognition sites. | J Med Chem 37: 2001-10 (1994) | Organix Inc | 2D 3D TSV |
8027982 | 19 | Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates. | J Med Chem 37: 1996-2000 (1994) | Pfizer Inc | 2D 3D TSV |
8027981 | 8 | Synthesis and characterization of selective fluorescent ligands for the neurokinin NK2 receptor. | J Med Chem 37: 1991-5 (1994) | Glaxo Institute for Molecular Biology | 2D 3D TSV |
8027978 | 50 | Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds. | J Med Chem 37: 1964-70 (1994) | Albany Molecular Research, Inc. | 2D 3D TSV |
8027974 | 98 | Influence of amine substituents on 5-HT2A versus 5-HT2C binding of phenylalkyl- and indolylalkylamines. | J Med Chem 37: 1929-35 (1994) | Virginia Commonwealth University | 2D 3D TSV |
8022403 | 113 | A binding site model and structure-activity relationships for the rat A3 adenosine receptor. | Mol Pharmacol 45: 1101-11 (1994) | National Institute of Diabetes, Digestive and Kidney Diseases | 2D 3D TSV |
8021931 | 19 | (6,7-Diaryldihydropyrrolizin-5-yl)acetic acids, a novel class of potent dual inhibitors of both cyclooxygenase and 5-lipoxygenase. | J Med Chem 37: 1894-7 (1994) | Merckle GmbH | 2D 3D TSV |
8021930 | 10 | (R)-methanandamide: a chiral novel anandamide possessing higher potency and metabolic stability. | J Med Chem 37: 1889-93 (1994) | University of Connecticut | 2D 3D TSV |
8021929 | 13 | Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety. | J Med Chem 37: 1886-8 (1994) | University of Minnesota | 2D 3D TSV |
8021926 | 41 | New thiol inhibitors of neutral endopeptidase EC 3.4.24.11: synthesis and enzyme active-site recognition. | J Med Chem 37: 1865-73 (1994) | University of Paris | 2D 3D TSV |
8021923 | 27 | A new series of photoactivatable and iodinatable linear vasopressin antagonists. | J Med Chem 37: 1841-9 (1994) | UPR 9023 CNRS | 2D 3D TSV |
8021921 | 28 | Dual angiotensin converting enzyme/thromboxane synthase inhibitors. | J Med Chem 37: 1823-32 (1994) | Ciba-Geigy Corporation | 2D 3D TSV |
8021920 | 87 | Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of disubstituted ureas and carbamates. Effects on ACAT inhibition in vitro and efficacy in vivo. | J Med Chem 37: 1810-22 (1994) | Parke-Davis Pharmaceutical Research | 2D 3D TSV |
8021917 | 84 | Three-dimensional pharmacophores from binding data. | J Med Chem 37: 1769-78 (1994) | Ciba-Geigy Corporation | 2D 3D TSV |
8021916 | 11 | Aminodiol HIV protease inhibitors. 1. Design, synthesis, and preliminary SAR. | J Med Chem 37: 1758-68 (1994) | Bristol-Myers Squibb Co. | 2D 3D TSV |
8021915 | 16 | Newly discovered stereochemical requirements in the side-chain conformation of delta opioid agonists for recognizing opioid delta receptors. | J Med Chem 37: 1746-57 (1994) | University of Arizona | 2D 3D TSV |
8021913 | 9 | Synthesis and characterization of [125I]-N-(N-benzylpiperidin-4-yl)-4- iodobenzamide, a new sigma receptor radiopharmaceutical: high-affinity binding to MCF-7 breast tumor cells. | J Med Chem 37: 1737-9 (1994) | George Washington University Medical Center | 2D 3D TSV |
8021912 | 7 | 2-Azetidinones as inhibitors of cholesterol absorption. | J Med Chem 37: 1733-6 (1994) | Schering-Plough Research Institute | 2D 3D TSV |
8012715 | 38 | GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. | Br J Pharmacol 111: 332-8 (1994) | Glaxo Group Research Ltd. | 2D 3D TSV |