PMID
Article Title
Citation
Organization
Download
View Data
Iloperidone binding to human and rat dopamine and 5-HT receptors.
Eur J Pharmacol 317: 417-23 (1996)
Hoechst Marion Roussel
Cloning, expression and pharmacological characterization of rabbit adenosine A1 and A3 receptors.
J Pharmacol Exp Ther 280: 122-8 (1997)
Pfizer
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
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
Two fungal lanostane derivatives as phospholipase A2 inhibitors.
J Nat Prod 59: 977-9 (1997)
Universitat De Val£Ncia
Structure-activity relationships of phomactin derivatives as platelet activating factor antagonists.
J Med Chem 39: 5281-4 (1997)
Sankyo
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
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
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
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
Synthesis and phospholipase A2 inhibitory activity of thielocin B3 derivatives.
J Med Chem 39: 5183-91 (1997)
Shionogi
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides.
J Med Chem 39: 5159-75 (1997)
Eli Lilly
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 2. Indole-3-acetamides with additional functionality.
J Med Chem 39: 5137-58 (1997)
Eli Lilly
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
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
Design, synthesis, and evaluation of nonpeptidic inhibitors of human rhinovirus 3C protease.
J Med Chem 39: 5072-82 (1997)
Agouron Pharmaceuticals
Structure-based alignment and comparative molecular field analysis of acetylcholinesterase inhibitors.
J Med Chem 39: 5064-71 (1997)
University Of North Carolina
Indole derivatives as a new class of steroid 5 alpha-reductase inhibitors.
J Med Chem 39: 5047-52 (1997)
Kyowa Hakko Kogyo
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
Identification of retinoic acid receptor beta subtype specific agonists.
J Med Chem 39: 5027-30 (1997)
Allergan
Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist.
J Pharmacol Exp Ther 279: 1392-403 (1996)
Pharmacia And Upjohn
The interaction of the enantiomers of aceclidine with subtypes of the muscarinic receptor.
J Pharmacol Exp Ther 279: 1335-44 (1996)
University Of California
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
Synthesis, biological activity, and molecular modeling of selective 5-HT(2C/2B) receptor antagonists.
J Med Chem 39: 4966-77 (1997)
Smithkline Beecham Pharmaceuticals
Potent 6-desfluoro-8-methylquinolones as new lead compounds in antibacterial chemotherapy.
J Med Chem 39: 4952-7 (1996)
Universit£
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
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
J Med Chem 39: 4935-41 (1997)
Drew University
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£
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
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
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
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
Development of potent thrombin receptor antagonist peptides.
J Med Chem 39: 4879-87 (1997)
Bristol-Myers Squibb Pharmaceutical Research Institute
(Carboxyalkyl)benzyl propargyl ethers as selective inhibitors of leukocyte-type 12-lipoxygenases.
J Med Chem 39: 4871-8 (1997)
Wayne State University
Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists.
J Med Chem 39: 4867-70 (1997)
Smithkline Beecham Pharmaceuticals
Reversal of P-glycoprotein-associated multidrug resistance by ivermectin.
Biochem Pharmacol 53: 17-25 (1997)
Institute Of Parasitology Of Mcgill University
Human dipeptide transporter, hPEPT1, stably transfected into Chinese hamster ovary cells.
Pharm Res 13: 1631-4 (1996)
University Of California San Francisco
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
Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.
FEBS Lett 398: 19-25 (1996)
Cnrs Upr 9023
Six lignans from Phyllanthus myrtifolius.
J Nat Prod 59: 1061-5 (1996)
National Taiwan University
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
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
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
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
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
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
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
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
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
J Med Chem 39: 4692-703 (1997)
Glaxo Wellcome
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Psychopharmacology (Berl) 124: 57-73 (1996)
Janssen Research Foundation
Pharmacokinetic/pharmacodynamic relationship of benzodiazepines in the direct cortical stimulation model of anticonvulsant effect.
J Pharmacol Exp Ther 279: 803-12 (1996)
Leiden University
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
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
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
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
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
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
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
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
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
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
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
Inactivation of a novel neuropeptide Y/peptide YY receptor gene in primate species.
J Biol Chem 271: 27217-20 (1996)
Yamanouchi Pharmaceutical
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
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
Discovery and optimization of nonpeptide HIV-1 protease inhibitors.
Bioorg Med Chem 4: 1401-10 (1996)
Parke-Davis Pharmaceutical Research
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
Head group analogs of arachidonylethanolamide, the endogenous cannabinoid ligand.
J Med Chem 39: 4515-9 (1996)
University Of Connecticut
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
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
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
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
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.
J Med Chem 39: 4421-9 (1996)
Uppsala University
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
Heterocyclic ureas: inhibitors of acyl-CoA:cholesterol O-acyltransferase as hypocholesterolemic agents.
J Med Chem 39: 4382-95 (1996)
Warner-Lambert
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
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
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
Characterisation of the specific binding of the histamine H3 receptor antagonist radioligand [3H]GR168320.
Eur J Pharmacol 311: 305-10 (1996)
Glaxo Research & Development
Thermodynamics of hydrogen bond and hydrophobic interactions in cyclodextrin complexes.
Biophys J 71: 2144-54 (1996)
Nih
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
Characterisation of the melanocortin 4 receptor by radioligand binding.
Pharmacol Toxicol 79: 161-5 (1996)
Uppsala University
Antineoplastic agents. 340. Isolation and structural elucidation of bryostatins 16-18.
J Nat Prod 59: 286-9 (1997)
Arizona State University
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
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
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
Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor.
Psychopharmacology (Berl) 126: 234-40 (1996)
University Of Turku
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
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
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
Structural determinants of substrates for the prostaglandin transporter PGT.
Mol Pharmacol 50: 738-42 (1996)
Albert Einstein College Of Medicine
Identification and characterization of novel somatostatin antagonists.
Mol Pharmacol 50: 709-15 (1996)
Cyenamid Agricultural Research Center
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
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
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
J Med Chem 39: 4299-312 (1996)
Dupont Pharmaceuticals
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
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
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
Novel potent sigma 1 ligands: N-[omega-(tetralin-1-yl)alkyl]piperidine derivatives.
J Med Chem 39: 4255-60 (1996)
Universit£
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£
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
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£
Structure-activity relationships for inhibition of inosine monophosphate dehydrogenase by nuclear variants of mycophenolic acid.
J Med Chem 39: 4181-96 (1996)
Syntex Research
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
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
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
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
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
Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay.
Anticancer Drugs 7: 568-78 (1997)
Strasbourg 1 University
A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines.
Life Sci 59: 1259-68 (1996)
Eli Lilly
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
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
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
New purines and purine analogs as modulators of multidrug resistance.
J Med Chem 39: 4099-108 (1996)
Institut De Recherches Servier
Novel peptidyl alpha-keto amide inhibitors of calpains and other cysteine proteases.
J Med Chem 39: 4089-98 (1996)
Georgia Institute Of Technology
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
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
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
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
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
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
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
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
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
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
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
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
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
Identification of a novel hypothalamic neuropeptide Y receptor associated with feeding behavior.
J Biol Chem 271: 26315-9 (1996)
Bayer
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
Radioreceptor binding profile of the atypical antipsychotic olanzapine.
Neuropsychopharmacology 14: 87-96 (1996)
Eli Lilly
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
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
[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
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
(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
A novel series of (phenoxyalkyl)imidazoles as potent H3-receptor histamine antagonists.
J Med Chem 39: 3806-13 (1996)
University College London
Unsaturated side chain beta-11-hydroxyhexahydrocannabinol analogs.
J Med Chem 39: 3790-6 (1996)
University Of Hawaii
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
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
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
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
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
Iodinated analogs of trimetoquinol as highly potent and selective beta 2-adrenoceptor ligands.
J Med Chem 39: 3701-11 (1996)
University Of Tennessee-Memphis
Synthesis and cardiotonic activity of novel pyrimidine derivatives: crystallographic and quantum chemical studies.
J Med Chem 39: 3671-83 (1996)
Università
Potent inhibitors of secretory phospholipase A2: synthesis and inhibitory activities of indolizine and indene derivatives.
J Med Chem 39: 3636-58 (1996)
Shionogi
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
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
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
GR127935: a potent and selective 5-HT1D receptor antagonist.
Behav Brain Res 73: 157-61 (1996)
Glaxo Research And Development
Novel discriminatory ligands for 5-HT2B receptors.
Behav Brain Res 73: 149-52 (1996)
Smithkline Beecham Pharmaceuticals
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
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
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
Synthesis and structure-activity relationships of retinoid X receptor selective diaryl sulfide analogs of retinoic acid.
J Med Chem 39: 3556-63 (1996)
Allergan
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
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
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
Nonlinear quantitative structure-activity relationship for the inhibition of dihydrofolate reductase by pyrimidines.
J Med Chem 39: 3526-32 (1996)
Scripps Research Institute
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
11-substituted (R)-aporphines: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions.
J Med Chem 39: 3503-13 (1996)
Uppsala University
10-substituted 11-oxygenated (R)-aporphines: synthesis, pharmacology, and modeling of 5-HT1A receptor interactions.
J Med Chem 39: 3491-502 (1996)
Uppsala University
Novel 5-aminoflavone derivatives as specific antitumor agents in breast cancer.
J Med Chem 39: 3461-9 (1996)
Kyowa Hakko Kogyo
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£
New series of potent, orally bioavailable, non-peptidic cyclic sulfones as HIV-1 protease inhibitors.
J Med Chem 39: 3431-4 (1996)
Gilead Sciences
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
Nigranoic acid, a triterpenoid from Schisandra sphaerandra that inhibits HIV-1 reverse transcriptase.
J Nat Prod 59: 525-7 (1996)
Chinese Academy Of Sciences
HIV inhibitory natural products. 26. Quinoline alkaloids from Euodia roxburghiana.
J Nat Prod 59: 469-71 (1996)
National Cancer Institute
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
Binding properties of somatostatin receptor subtypes.
Metab Clin Exp 45: 17-20 (1996)
Sandoz Pharma
(+/-)-3-[4'-(N,N-dimethylamino)cinnamyl]benzazepine analogs: novel dopamine D1 receptor antagonists.
J Med Chem 39: 3423-8 (1996)
National Institutes Of Health
Design, synthesis, and biological evaluation of ellipticine-estradiol conjugates.
J Med Chem 39: 3367-74 (1996)
Purdue University
Mechanistic studies on the inactivation of papain by epoxysuccinyl inhibitors.
J Med Chem 39: 3357-66 (1996)
University Of Wisconsin
New low-density lipoprotein receptor upregulators acting via a novel mechanism.
J Med Chem 39: 3343-56 (1996)
RhôNe-Poulenc Rorer
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
Paracyclophanes: a novel class of water-soluble inhibitors of HIV proteinase.
J Med Chem 39: 3291-9 (1996)
Sandoz Research Institute
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
3-(2-Benzofuranyl)quinuclidin-2-ene derivatives: novel muscarinic antagonists.
J Med Chem 39: 3269-77 (1996)
Uppsala University
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
Structural modifications of thalidomide produce analogs with enhanced tumor necrosis factor inhibitory activity.
J Med Chem 39: 3238-40 (1996)
Celgene
(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
Identification of the first retinoid X, receptor homodimer antagonist.
J Med Chem 39: 3229-34 (1996)
Ligand Pharmaceuticals
Aza-peptide analogs as potent human immunodeficiency virus type-1 protease inhibitors with oral bioavailability.
J Med Chem 39: 3203-16 (1996)
Ciba-Geigy
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£
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
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
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
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
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
Orally active fibrinogen receptor antagonists. 2. Amidoximes as prodrugs of amidines.
J Med Chem 39: 3139-47 (1996)
F. Hoffmann-La Roche
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
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
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
Mechanism-based inhibition of L-pipecolate oxidase by 4,5-dehydro-L-pipecolic acid.
J Med Chem 39: 3046-8 (1996)
Oregon State University
Potent inhibition of tumor necrosis factor-alpha production by tetrafluorothalidomide and tetrafluorophthalimides.
J Med Chem 39: 3044-5 (1996)
Institute Of Technology
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
Identification of a retinoic acid receptor alpha subtype specific agonist.
J Med Chem 39: 3035-8 (1996)
Allergan
Lycaconitine revisited: partial synthesis and neuronal nicotinic acetylcholine receptor affinities.
J Nat Prod 59: 707-9 (1996)
Ohio Northern University
Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist.
Br J Pharmacol 117: 1558-64 (1996)
University Of Occupational And Environmental Health
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
Anti-influenza virus activities of 4-substituted 2,4-dioxobutanoic acid inhibitors.
Antimicrob Agents Chemother 40: 1304-7 (1996)
Merck Research Laboratories
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
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
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
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
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
Synthesis and activity of a novel series of 3-biarylquinuclidine squalene synthase inhibitors.
J Med Chem 39: 2971-9 (1996)
Zeneca Pharmaceuticals
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
Similarities and differences in the structure-activity relationships of capsaicin and resiniferatoxin analogues.
J Med Chem 39: 2939-52 (1996)
Institute For Medical Research
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£
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
(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
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
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
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
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
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
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
Forskolin carbamates: binding and activation studies with type I adenylyl cyclase.
J Med Chem 39: 2745-52 (1996)
Food And Drug Administration
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
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
Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity.
J Med Chem 39: 2672-80 (1996)
Universitá
(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
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
J Med Chem 39: 2659-63 (1996)
Ligand Pharmaceuticals
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
Modulators of leukotriene biosynthesis and receptor activation.
J Med Chem 39: 2629-54 (1996)
Abbott Laboratories
Effect of Polygonum hydropiper sulfated flavonoids on lens aldose reductase and related enzymes.
J Nat Prod 59: 443-5 (1996)
Fukuyama University
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
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
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
A structure-activity relationship study of novel phenylacetamides which are sodium channel blockers.
J Med Chem 39: 1514-20 (1996)
Warner-Lambert
trans-2-Aryl-N,N-dipropylcyclopropylamines: synthesis and interactions with 5-HT(1A) receptors.
J Med Chem 39: 1485-93 (1996)
Uppsala University
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
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
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
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
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
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
Geranylgeranyl diphosphate-based inhibitors of post-translational geranylgeranylation of cellular proteins.
J Med Chem 39: 1352-6 (1996)
Università
Active site directed inhibition of estrone sulfatase by nonsteroidal coumarin sulfamates.
J Med Chem 39: 1349-51 (1996)
University Of Bath
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
Alkyl and alkoxyethyl antineoplastic phospholipids.
J Med Chem 39: 2609-14 (1996)
National Hellenic Research Foundation
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
Synthesis and biological activity of 3- and 5-amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone.
J Med Chem 39: 2586-93 (1996)
Yale University
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
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
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
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
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
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
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
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
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
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
(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
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
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
New neplanocin analogues. 6. Synthesis and potent antiviral activity of 6'-homoneplanocin A1.
J Med Chem 39: 2392-9 (1996)
Hokkaido University
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
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
Aristeromycin-5'-carboxaldehyde: a potent inhibitor of S-adenosyl-L-homocysteine hydrolase.
J Med Chem 39: 2347-53 (1996)
University Of Kansas
Ryanodine action at calcium release channels. 2. relation to substituents of the cyclohexane ring.
J Med Chem 39: 2339-46 (1996)
University Of California
Ryanodine action at calcium release channels. 1. importance of hydroxyl substituents.
J Med Chem 39: 2331-8 (1996)
University Of California
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
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
Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
J Med Chem 39: 2293-301 (1996)
National Institute Of Diabetes
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
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
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
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
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
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
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
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
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
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
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
Carbohydrates in an acidic multivalent assembly: nanomolar P-selectin inhibitors.
J Med Chem 39: 1018-20 (1996)
Lawrence Berkeley National Laboratories
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
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
Effects of Various Isoquinoline Alkaloids on In Vitro 3H-Dopamine Uptake by Rat Striatal Synaptosomes
J Nat Prod 58: 1475-1484 (1995)
TBA
ATP-dependent glutathione disulphide transport mediated by the MRP gene-encoded conjugate export pump.
Biochem J 314: 433-7 (1996)
Deutsches Krebsforschungszentrum
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
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
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
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
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
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
Comparative molecular moment analysis (CoMMA): 3D-QSAR without molecular superposition.
J Med Chem 39: 2129-40 (1996)
Ibm Thomas J. Watson Research Center
Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.
J Med Chem 39: 2123-8 (1996)
Basf
Discovery of an orally active non-peptide fibrinogen receptor antagonist.
J Med Chem 39: 2118-22 (1996)
Hoechst
The C-terminal domain of the mGluR1 metabotropic glutamate receptor affects sensitivity to agonists.
J Neurochem 67: 58-63 (1996)
Cns Research
Similarity between rat brain nicotinic alpha-bungarotoxin receptors and stably expressed alpha-bungarotoxin binding sites.
J Neurochem 67: 145-54 (1996)
Mcgill University
Cloning and expression of a novel neuropeptide Y receptor.
J Biol Chem 271: 16435-8 (1996)
Merck Research Laboratories
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
Inhibitors of acyl CoA:cholesterol acyltransferase.
J Med Chem 39: 1704-19 (1996)
Schering-Plough Research Institute
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
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
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
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
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
Conformationally restricted TRH analogs: a probe for the pyroglutamate region.
J Med Chem 39: 1571-4 (1996)
Washington University
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
Design and synthesis of new linear and cyclic bradykinin antagonists.
J Med Chem 39: 2095-101 (1996)
Institute De Recherches Servier
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
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
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£
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
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
Discovery of novel, non-peptide HIV-1 protease inhibitors by pharmacophore searching.
J Med Chem 39: 2047-54 (1996)
National Institutes Of Health
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
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
(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
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
Design and synthesis of 2-naphthoate esters as selective dopamine D4 antagonists.
J Med Chem 39: 1946-8 (1996)
Smithkline Beecham Pharmaceuticals
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
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
Transport of glutathione, glucuronate, and sulfate conjugates by the MRP gene-encoded conjugate export pump.
Cancer Res 56: 988-94 (1996)
Deutsches Krebsforschungszentrum
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
Studies on selectin blocker. 1. Structure-activity relationships of sialyl Lewis X analogs.
J Med Chem 39: 1339-43 (1996)
Institute Of Cancer Research
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
Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers.
J Med Chem 39: 1303-13 (1996)
Medichem Research
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
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
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
[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
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
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
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
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
Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.
J Med Chem 39: 982-91 (1996)
Abbott Laboratories
Azole endothelin antagonists. 2. Structure-activity studies.
J Med Chem 39: 968-81 (1996)
Abbott Laboratories
Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile.
J Med Chem 39: 957-67 (1996)
Abbott Laboratories
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
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
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
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
Comparative molecular field analysis-based prediction of drug affinities at recombinant D1A dopamine receptors.
J Med Chem 39: 850-9 (1996)
Va Medical Center
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
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
(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
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
Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences.
J Pharmacol Exp Ther 276: 720-7 (1996)
Eli Lilly
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
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
2-(Hydroxyalkyl)estradiols: synthesis and biological evaluation.
J Med Chem 39: 1917-23 (1996)
Ohio State University
Structure-based design of novel, urea-containing FKBP12 inhibitors.
J Med Chem 39: 1872-84 (1996)
Agouron Pharmaceuticals
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
Novel terphenyls as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents.
J Med Chem 39: 1846-56 (1996)
Searle Research And Development
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
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
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
Non-peptide cholecystokinin-B/gastrin receptor antagonists based on bicyclic, heteroaromatic skeletons.
J Med Chem 39: 1806-15 (1996)
James Black Foundation
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
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
J Med Chem 39: 1778-89 (1996)
Ligand Pharmaceuticals
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
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
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
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
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
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
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
Novel N6-(substituted-phenylcarbamoyl)adenosine-5'-uronamides as potent agonists for A3 adenosine receptors.
J Med Chem 39: 802-6 (1996)
Universit£
Interactions of flavonoids and other phytochemicals with adenosine receptors.
J Med Chem 39: 781-8 (1996)
National Institute Of Diabetes
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
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
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
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
J Med Chem 39: 736-48 (1996)
Eli Lilly
Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
J Med Chem 39: 713-9 (1996)
Glaxo Wellcome Research Institute
Quinazoline antifolates thymidylate synthase inhibitors: lipophilic analogues with modification to the C2-methyl substituent.
J Med Chem 39: 695-704 (1996)
Zeneca Pharma
Slow-binding inhibition of gamma-aminobutyric acid aminotransferase by hydrazine analogues.
J Med Chem 39: 686-94 (1996)
Northwestern University
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
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
alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase.
J Med Chem 39: 657-60 (1996)
Bristol-Myers Squibb Pharmaceutical Research Institute
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
J Med Chem 39: 625-56 (1996)
Dupont Pharmaceuticals
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
(-)-Arctigenin as a lead structure for inhibitors of human immunodeficiency virus type-1 integrase.
J Med Chem 39: 86-95 (1996)
Freie UniversitäT Berlin
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
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
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
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
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
Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors.
J Med Chem 39: 314-22 (1996)
Virginia Commonwealth University
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
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
Conformational analysis of D1 dopamine receptor agonists: pharmacophore assessment and receptor mapping.
J Med Chem 39: 285-96 (1996)
University Of North Carolina
Theoretical study of inhibition of adenosine deaminase by (8R)-coformycin and (8R)-deoxycoformycin.
J Med Chem 39: 277-84 (1996)
University Of California
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
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
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
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
Design and synthesis of non-peptide Ras CAAX mimetics as potent farnesyltransferase inhibitors.
J Med Chem 39: 217-23 (1996)
University Of Pittsburgh
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
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
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
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.
J Med Chem 39: 176-82 (1996)
Universit£
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
Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives.
J Med Chem 39: 149-57 (1996)
Glaxo Wellcome
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
J Med Chem 39: 143-8 (1996)
Pfizer
Structure-antigastrin activity relationships of new spiroglumide amido acid derivatives.
J Med Chem 39: 135-42 (1996)
Rotta Research Laboratorium
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£
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
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
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
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
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
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
Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
J Med Chem 39: 582-7 (1996)
Hoechst-Roussel Pharmaceuticals
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
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
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
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
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
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
Tetrahydrobenzothiophenone derivatives as a novel class of adenosine receptor antagonists.
J Med Chem 39: 398-406 (1996)
National Institute Of Diabetes
A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease.
J Med Chem 39: 392-7 (1996)
Abbott Laboratories
A comparative molecular field analysis study of N-benzylpiperidines as acetylcholinesterase inhibitors.
J Med Chem 39: 380-7 (1996)
University Of Missouri St. Louis
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
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
Potent, cell active, non-thiol tetrapeptide inhibitors of farnesyltransferase.
J Med Chem 39: 353-8 (1996)
Bristol-Myers Squibb Pharmaceutical Research Institute
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
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
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
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
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
Synthesis, structure-affinity relationships, and biological activities of ligands binding to retinoic acid receptor subtypes.
J Med Chem 38: 4993-5006 (1996)
Cird Galderma
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
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
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
Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors.
J Med Chem 38: 4968-71 (1995)
Upjohn
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
D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs.
Psychopharmacology (Berl) 120: 365-8 (1995)
Case Western Reserve University
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.
J Med Chem 38: 4950-2 (1996)
Neurogen
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
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.
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
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
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
Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
J Neurochem 66: 47-56 (1996)
University Of Washington
Molecular biology of somatostatin receptors.
Endocr Rev 16: 427-42 (1995)
University Of Pennsylvania
(+/-) 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
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
Multiple binding modes for the receptor-bound conformations of cyclic AII agonists.
J Med Chem 36: 1902-13 (1993)
Washington University
Inhibition and inactivation of presynaptic cholinergic markers using redox-reactive choline analogs.
J Med Chem 36: 1893-901 (1993)
University Of Toledo
Potent nonpeptide angiotensin II receptor antagonists. 2. 1-(Carboxybenzyl)imidazole-5-acrylic acids.
J Med Chem 36: 1880-92 (1993)
Smithkline Beecham Pharmaceuticals
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
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
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
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
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
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
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
5-HT3 receptor antagonists. 2. 4-Hydroxy-3-quinolinecarboxylic acid derivatives.
J Med Chem 36: 617-26 (1993)
Kyowa Hakko Kogyo
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
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
Synthesis of 2-imidazolidinylidenepropanedinitrile derivatives as stimulators of gastrointestinal motility.
J Med Chem 36: 572-9 (1993)
Kyowa Hakko Kogyo
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
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
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
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
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
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
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
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
(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)
N-(arylalkyl)farnesylamines: new potent squalene synthetase inhibitors.
J Med Chem 36: 1501-4 (1993)
Sandoz Research Institute
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
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
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
Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds.
J Med Chem 36: 1393-400 (1993)
Ciba-Geigy
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
J Med Chem 36: 1380-6 (1993)
Hokuriku University
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
Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists.
J Med Chem 36: 1333-42 (1993)
National Institute Of Diabetes
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
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
The Role of Receptor Binding in Drug Discovery
J Nat Prod 56: 441-455 (1993)
TBA
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
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
New indole derivatives as potent and selective serotonin uptake inhibitors.
J Med Chem 36: 1194-202 (1993)
Centre De Recherches De Vitry-Alfortville
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
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£
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
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£
Nonsymmetrical bipiperidyls as inhibitors of vesicular acetylcholine storage.
J Med Chem 36: 985-9 (1993)
University Of Minnesota
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
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
Inhibition studies of some serine and thiol proteinases by new leupeptin analogues.
J Med Chem 36: 1084-9 (1993)
University Of Arkansas
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
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
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
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
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
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
Bicyclic compounds as ring-constrained inhibitors of protein-tyrosine kinase p56lck.
J Med Chem 36: 425-32 (1993)
National Cancer Institute-Bethesda
Cannabinoid structure-activity relationships: correlation of receptor binding and in vivo activities.
J Pharmacol Exp Ther 265: 218-26 (1993)
Virginia Commonwealth University
Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors.
J Med Chem 36: 924-7 (1993)
Merck Research Laboratories
Adenosine-5'-carboxaldehyde: a potent inhibitor of S-adenosyl-L-homocysteine hydrolase.
J Med Chem 36: 883-7 (1993)
University Of Kansas
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
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
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
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
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
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
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
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
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
32-Methyl-32-oxylanosterols: dual-action inhibitors of cholesterol biosynthesis.
J Med Chem 36: 410-6 (1993)
Institute
Defining structural requirements for neuropeptide Y receptors using truncated and conformationally restricted analogues.
J Med Chem 36: 385-93 (1993)
Salk Institute
Inhibition of the tetracycline efflux antiport protein by 13-thio-substituted 5-hydroxy-6-deoxytetracyclines.
J Med Chem 36: 370-7 (1993)
Tufts University
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
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
Highly selective tripeptide thrombin inhibitors.
J Med Chem 36: 314-9 (1993)
Eli Lilly
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
LY248686, a new inhibitor of serotonin and norepinephrine uptake.
Neuropsychopharmacology 8: 23-33 (1993)
Eli Lilly
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
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
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
(+)-Hemipalmitoylcarnitinium strongly inhibits carnitine palmitoyltransferase-I in intact mitochondria.
J Med Chem 36: 237-42 (1993)
Louisiana State University
Development of selective tight-binding inhibitors of leukotriene A4 hydrolase.
J Med Chem 36: 211-20 (1993)
Scripps Research Institute
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
Structural determinants of haloenol lactone-mediated suicide inhibition of canine myocardial calcium-independent phospholipase A2.
J Med Chem 36: 95-100 (1993)
Washington University
Exploration of neutral endopeptidase active site by a series of new thiol-containing inhibitors.
J Med Chem 36: 87-94 (1993)
University Of Paris
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
S-adenosylmethionine decarboxylase inhibitors: new aryl and heteroaryl analogues of methylglyoxal bis(guanylhydrazone).
J Med Chem 36: 46-54 (1993)
Ciba-Geigy
Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction.
J Med Chem 36: 21-9 (1993)
Roche Products
Hemicholinium and related lipids: inhibitors of protein kinase C.
J Med Chem 36: 177-8 (1993)
Louisiana State University
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
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
Nonpeptide angiotensin II antagonists: N-phenyl-1H-pyrrole derivatives are angiotensin II receptor antagonists.
J Med Chem 36: 101-10 (1993)
Searle
[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
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
Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor.
J Med Chem 36: 3032-4 (1993)
Hebrew University
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
Hydroxylated 2-(5'-salicyl)naphthalenes as protein-tyrosine kinase inhibitors.
J Med Chem 36: 3015-20 (1993)
National Institutes Of Health
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
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.
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
Synthesis and protein-tyrosine kinase inhibitory activity of polyhydroxylated stilbene analogues of piceatannol.
J Med Chem 36: 2950-5 (1993)
Purdue University
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
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
2-Amido-8-methoxytetralins: a series of nonindolic melatonin-like agents.
J Med Chem 36: 2891-8 (1993)
University Of Groningen
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
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
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
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
J Med Chem 36: 2842-50 (1993)
Eli Lilly
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
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
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
Renin inhibitors containing a pyridyl amino diol derived C-terminus.
J Med Chem 36: 2788-800 (1993)
Hoechst
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
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
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
Novel antagonists of 5-HT3 receptors. Synthesis and biological evaluation of piperazinylquinoxaline derivatives.
J Med Chem 36: 2745-50 (1993)
Universidad De Navarra
(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
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
Plant antitumor agents. 30. Synthesis and structure activity of novel camptothecin analogs.
J Med Chem 36: 2689-700 (1993)
Research Triangle Institute
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
J Med Chem 36: 2676-88 (1993)
Abbott Laboratories
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
Effect of trifluoromethyl and other substituents on activity of xanthines at adenosine receptors.
J Med Chem 36: 2639-44 (1993)
National Institutes Of Health
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
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
Structure-activity relationships of C-terminal endothelin hexapeptide antagonists.
J Med Chem 36: 2585-94 (1993)
Warner-Lambert
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
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
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
Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Mol Pharmacol 44: 229-36 (1993)
Cnrs
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
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
Design of potent, cyclic peptide bradykinin receptor antagonists from conformationally constrained linear peptides.
J Med Chem 36: 2569-71 (1993)
Scios Nova
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
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
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
N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.
J Med Chem 36: 2044-5 (1993)
Merck Sharp And Dohme Research Laboratories
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
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
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
Non-peptide ligands for opioid receptors. Design of kappa-specific agonists.
J Med Chem 36: 1860-5 (1993)
Universit£
Design, synthesis, and pharmacological evaluation of potent xanthone dicarboxylic acid leukotriene B4 receptor antagonists.
J Med Chem 36: 1726-34 (1993)
Eli Lilly
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
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
NMR and computational evidence that high-affinity bradykinin receptor antagonists adopt C-terminal beta-turns.
J Med Chem 36: 1450-60 (1993)
Scios Nova
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
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
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
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
Bioactive ryanoids from nucleophilic additions to 4,12-seco-4,12-dioxoryanodine.
J Med Chem 36: 1128-35 (1993)
University Of California
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
The effect of NMeTyr5 substitution in luteinizing hormone-releasing hormone antagonists.
J Med Chem 36: 928-33 (1993)
Abbott Laboratories
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
Synthesis and anti-HIV evaluation of D4T and D4T 5'-monophosphate prodrugs.
J Med Chem 36: 826-30 (1993)
Ura Cnrs 1309
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
A topochemical approach to explain morphiceptin bioactivity.
J Med Chem 36: 708-19 (1993)
University Of California
A new bastadin from the sponge Psammaplysilla purpurea.
J Nat Prod 56: 153-7 (1993)
University Of Hawaii
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
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
Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase.
J Med Chem 36: 421-3 (1993)
Eli Lilly
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
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.
J Med Chem 36: 363-9 (1993)
Abbott Laboratories
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
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
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
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
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
A mechanism-based inactivation study of neutral endopeptidase 24.11.
J Med Chem 36: 2408-11 (1993)
Salk Biotechnology/Industrial Associates
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
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
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
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
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
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
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
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
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
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
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
Peptidomimetic HIV protease inhibitors: phosphate prodrugs with improved biological activities.
J Med Chem 36: 2575-7 (1993)
Upjohn
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
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
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
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
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
Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering.
J Med Chem 36: 2235-7 (1993)
Syntex Discovery Research
Synthesis and antitumor activity of 10-propargyl-10-deazaaminopterin.
J Med Chem 36: 2228-31 (1993)
Sri International
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
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazolecarboxylic acids.
J Med Chem 36: 2182-95 (1993)
Takeda Chemical Industries
Synthesis and structure-activity relationships of nonpeptide, potent triazolone-based angiotensin II receptor antagonists.
J Med Chem 36: 2172-81 (1993)
Searle R&D
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
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
Sulfonylmethanesulfonamide inhibitors of carbonic anhydrase.
J Med Chem 36: 2134-41 (1993)
Merck Research Laboratories
(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
Excursions in drug discovery.
J Med Chem 36: 2051-8 (1993)
Merck Research Laboratories
Synthesis and biological evaluation of antiplatelet 2-aminochromones.
J Med Chem 36: 2026-32 (1993)
Upjohn Laboratories
Characteristics of histamine H1 receptors on HeLa cells.
Eur J Pharmacol 245: 291-5 (1993)
University Of Cambridge
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
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
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
CNAD: a potent and specific inhibitor of alcohol dehydrogenase.
J Med Chem 37: 392-9 (1994)
University Of Rochester Medical Center
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
Bound water molecules and conformational stabilization help mediate an antigen-antibody association.
Proc Natl Acad Sci U S A 91: 1089-93 (1994)
Institut Pasteur
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
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
Expression and pharmacological characterization of the human D3 dopamine receptor.
J Pharmacol Exp Ther 268: 417-26 (1994)
Neuroscience Research Centre
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
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
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
Tetrapeptide CCK agonists: structure-activity studies on modifications at the N-terminus.
J Med Chem 37: 309-13 (1994)
Abbott Laboratories
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
Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors.
J Med Chem 37: 293-304 (1994)
Upjohn Laboratories
Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers.
J Med Chem 37: 268-74 (1994)
Warner-Lambert
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
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
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
Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential.
J Med Chem 37: 219-21 (1994)
University Of Bath
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
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
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
A recombinant human stromelysin catalytic domain identifying tryptophan derivatives as human stromelysin inhibitors.
J Med Chem 37: 206-9 (1994)
Warner-Lambert
Adenosine deaminase inhibitors: synthesis and structure-activity relationships of 2-hydroxy-3-nonyl derivatives of azoles.
J Med Chem 37: 201-5 (1994)
Universit£
New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C.
J Med Chem 37: 195-200 (1994)
University Of North Carolina
Isozyme-specific glutathione-S-transferase inhibitors: design and synthesis.
J Med Chem 37: 189-94 (1994)
Terrapin Technologies
Synthesis of novel N-phosphonoalkyl dipeptide inhibitors of human collagenase.
J Med Chem 37: 158-69 (1994)
Smithkline Beecham Pharmaceuticals
Interaction of tetrahydrostilbazoles with monoamine oxidase A and B.
J Med Chem 37: 151-7 (1994)
University Of California
Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.
J Med Chem 37: 146-50 (1994)
University Of Arizona
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
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
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
Zaragozic Acids D and D2: Potent Inhibitors of Squalene Synthase and of Ras Farnesyl-Protein Transferase
J Nat Prod 56: 1923-1929 (1993)
TBA
Evaluation of 5-[18F]fluoropropylepidepride as a potential PET radioligand for imaging dopamine D2 receptors.
Synapse 15: 169-76 (1993)
Vanderbilt University
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
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
Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides.
J Med Chem 36: 4293-301 (1994)
Merck Research Laboratories
Development of 1,4-benzodiazepine cholecystokinin type B antagonists.
J Med Chem 36: 4276-92 (1994)
Merck Research Laboratories
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
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
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
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
Kinase inhibitors from Polygonum cuspidatum.
J Nat Prod 56: 1805-10 (1993)
Purdue University
Molecular cloning, expression, and pharmacological characterization of humEAA1, a human kainate receptor subunit.
J Neurochem 62: 1-9 (1994)
Allelix Biopharmaceuticals
(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
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
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
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
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
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
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
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
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
Synthesis of novel modified dipeptide inhibitors of human collagenase: beta-mercapto carboxylic acid derivatives.
J Med Chem 36: 4030-9 (1994)
Smithkline Beecham Pharmaceuticals
Xanthines with C8 chiral substituents as potent and selective adenosine A1 antagonists.
J Med Chem 36: 4015-20 (1994)
Marion Merrell Dow Research Institute
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
Nanomolar-affinity, non-peptide oxytocin receptor antagonists.
J Med Chem 36: 3993-4005 (1994)
Merck Research Laboratories
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
Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists.
J Med Chem 36: 3982-4 (1994)
Eli Lilly
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
3,4-Dihydroxychalcones as potent 5-lipoxygenase and cyclooxygenase inhibitors.
J Med Chem 36: 3904-9 (1994)
Tokushima Bunri University
R2 C-terminal peptide inhibition of mammalian and yeast ribonucleotide reductase.
J Med Chem 36: 3859-62 (1994)
University Of Pennsylvania
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
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
Heterocyclic lactam derivatives as dual angiotensin converting enzyme and neutral endopeptidase 24.11 inhibitors.
J Med Chem 36: 3829-33 (1994)
Ciba-Geigy
Design and synthesis of an orally active macrocyclic neutral endopeptidase 24.11 inhibitor.
J Med Chem 36: 3821-8 (1994)
Ciba-Geigy
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
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
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
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
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
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
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
(Dipropylphenoxy)phenylacetic acids: a new generation of nonpeptide angiotensin II receptor antagonists.
J Med Chem 36: 3738-42 (1994)
Merck Research Laboratories
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
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
18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography.
J Med Chem 36: 3707-20 (1994)
University Of Pennsylvania
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
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
Possible contribution of a glutathione conjugate to the long-duration action of beta-funaltrexamine.
J Med Chem 36: 3669-73 (1994)
University Of Minnesota
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
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
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
Transformation of heterocyclic reversible monoamine oxidase-B inactivators into irreversible inactivators by N-methylation.
J Med Chem 36: 3606-10 (1994)
Northwestern University
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
Substituted chromenes as potent, orally active 5-lipoxygenase inhibitors.
J Med Chem 36: 3580-94 (1994)
Ciba-Geigy
Analysis of cocaine receptor site ligand binding by three-dimensional Voronoi site modeling approach.
J Med Chem 36: 3572-9 (1994)
University Of Michigan
The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.
J Med Chem 36: 3533-41 (1994)
Medical Research Division Of American Cyanamid
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
[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
Molecular cloning and characterization of the human A3 adenosine receptor.
Proc Natl Acad Sci U S A 90: 10365-9 (1993)
Merck Research Laboratories
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
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
9-[(Phosphonoalkyl)benzyl]guanines. Multisubstrate analogue inhibitors of human erythrocyte purine nucleoside phosphorylase.
J Med Chem 36: 3455-63 (1993)
Burroughs Wellcome
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
New adenosine kinase inhibitors with oral antiinflammatory activity: synthesis and biological evaluation.
J Med Chem 36: 3424-30 (1993)
University Of California
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
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
A new series of imidazolones: highly specific and potent nonpeptide AT1 angiotensin II receptor antagonists.
J Med Chem 36: 3371-80 (1993)
Sanofi Recherche
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
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
Trisubstituted pyridine leukotriene B4 receptor antagonists: synthesis and structure-activity relationships.
J Med Chem 36: 3321-32 (1993)
Smithkline Beecham Pharmaceuticals
Synthesis of structural analogs of leukotriene B4 and their receptor binding activity.
J Med Chem 36: 3308-20 (1993)
Smithkline Beecham Pharmaceuticals
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
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
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
A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor.
J Med Chem 36: 3207-10 (1993)
Merck Research Laboratories
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
J Med Chem 36: 3188-96 (1993)
University Of GöTeborg
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
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
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
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
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
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
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
Conformationally restrained analogs of sympathomimetic catecholamines. Synthesis, conformational analysis, and adrenergic activity of isochroman derivatives.
J Med Chem 36: 3077-86 (1993)
Universit£
Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
J Biol Chem 268: 23422-6 (1993)
Synaptic Pharmaceutical
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
Molecular similarity, quantitative chirality, and QSAR for chiral drugs.
J Med Chem 37: 1727-32 (1994)
University Of Oxford
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£
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£
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£
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
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
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
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
Synthesis and carbonic anhydrase inhibitory activity of 4-substituted 2-thiophenesulfonamides.
J Med Chem 37: 1646-51 (1994)
Allergan
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
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
[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
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
Novel Asp32-replacement tetrapeptide analogues as potent and selective CCK-A agonists.
J Med Chem 37: 1562-8 (1994)
Abbott Laboratories
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
1,3-Diarylindan-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists.
J Med Chem 37: 1553-7 (1994)
Smithkline Beecham Pharmaceuticals
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
125I-4-aminobenzyl-5'-N-methylcarboxamidoadenosine, a high affinity radioligand for the rat A3 adenosine receptor.
Mol Pharmacol 45: 978-82 (1994)
Duke University
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
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
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
Search for the pharmacophore of bispyridinium-type allosteric modulators of muscarinic receptors.
J Med Chem 37: 1439-45 (1994)
University Of Bonn
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£
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
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
Protein kinase C. Modeling of the binding site and prediction of binding constants.
J Med Chem 37: 1326-38 (1994)
National Cancer Institute-Bethesda
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
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
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
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
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
Design of orally active, non-peptidic inhibitors of human leukocyte elastase.
J Med Chem 37: 1259-61 (1994)
Zeneca Pharmaceuticals Group
Potent, selective, and systemically-available inhibitors of acyl-coenzyme A:cholesterol acyl transferase (ACAT).
J Med Chem 37: 1252-5 (1994)
Pfizer
Applications of combinatorial technologies to drug discovery. 1. Background and peptide combinatorial libraries.
J Med Chem 37: 1233-51 (1994)
Affymax Research Institute
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
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
Characterization of a 5-hydroxytryptamine receptor in mouse neuroblastoma N18TG2 cells.
J Pharmacol Exp Ther 269: 246-55 (1994)
University Of Pennsylvania
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
Structural features important for sigma 1 receptor binding.
J Med Chem 37: 1214-9 (1994)
Virginia Commonwealth University
Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors.
J Med Chem 37: 1200-7 (1994)
Daiichi Pharmaceutical
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
Classical and nonclassical furo[2,3-d]pyrimidines as novel antifolates: synthesis and biological activities.
J Med Chem 37: 1169-76 (1994)
Duquesne University
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
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
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
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
Structure-based design of inhibitors of purine nucleoside phosphorylase. 4. A study of phosphate mimics.
J Med Chem 37: 1109-14 (1994)
Ciba-Geigy
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
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
J Med Chem 37: 1035-54 (1994)
Abbott Laboratories
Melatonin receptors: localization, molecular pharmacology and physiological significance.
Neurochem Int 24: 101-46 (1994)
Rowett Research Institute
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
Verongamine, a Novel Bromotyrosine-Derived Histamine H3-Antagonist from the Marine Sponge Verongula gigantea
J Nat Prod 57: 175-177 (1994)
TBA
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
Antiinflammatory 4,5-diarylpyrroles: synthesis and QSAR.
J Med Chem 37: 988-98 (1994)
Dupont Pharmaceuticals
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
Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase.
J Med Chem 37: 1015-27 (1994)
Ciba-Geigy
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
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
Benzo[f]quinazoline inhibitors of thymidylate synthase: methyleneamino-linked aroylglutamate derivatives.
J Med Chem 37: 838-44 (1994)
Wellcome Research Laboratories
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
Molecular modeling studies of aldose reductase inhibitors.
J Med Chem 37: 787-92 (1994)
National Eye Institute
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
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
Pseudopeptide inhibitors of Ras farnesyl-protein transferase.
J Med Chem 37: 725-32 (1994)
Merck Research Laboratories
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
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
3-Alkoxybenzo[b]thiophene-2-carboxamides as inhibitors of neutrophil-endothelial cell adhesion.
J Med Chem 37: 717-8 (1994)
Warner-Lambert
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
J Med Chem 37: 689-95 (1994)
Centre De Recherche Pierre Fabre MéDicament
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
Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases.
J Med Chem 37: 665-73 (1994)
University Of California
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£
Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists.
J Med Chem 37: 636-46 (1994)
National Institute Of Diabetes
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
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
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
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
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
Discovery of new non-phospholipid inhibitors of the secretory phospholipases A2.
J Med Chem 37: 557-9 (1994)
Fisons
Antiviral enantiomeric preference for 5'-noraristeromycin.
J Med Chem 37: 551-4 (1994)
University Of South Florida
Pyrido[2,3-d]pyrimidine angiotensin II antagonists.
J Med Chem 37: 542-50 (1994)
Wyeth-Ayerst Research
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
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
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
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
J Med Chem 37: 476-85 (1994)
Smithkline Beecham Pharmaceuticals
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
Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Mol Pharmacol 45: 330-4 (1994)
University Of Pennsylvania
Non-amine based analogues of lavendustin A as protein-tyrosine kinase inhibitors.
J Med Chem 36: 3010-4 (1993)
National Institutes Of Health
Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications.
Eur J Pharmacol 236: 483-6 (1993)
Maryland Psychiatric Research Center
Characterization of cloned somatostatin receptors SSTR4 and SSTR5.
Mol Pharmacol 44: 385-92 (1993)
University Of Pennsylvania
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
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
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.
J Med Chem 36: 2107-14 (1993)
University Of LièGe
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
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
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
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
Synthesis of isosteric analogues of nicotinamide adenine dinucleotide containing C-nucleotide of nicotinamide or picolinamide.
J Med Chem 36: 1855-9 (1993)
Cornell University
Unique binding characteristics of antipsychotic agents interacting with human dopamine D2A, D2B, and D3 receptors.
Mol Pharmacol 43: 749-54 (1993)
Astra Arcus
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
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
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
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
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
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
Dopamine D4 receptors bind inactive (+)-aporphines, suggesting neuroleptic role. Sulpiride not stereoselective.
Eur J Pharmacol 233: 173-4 (1993)
University Of Toronto
Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system.
J Med Chem 36: 912-8 (1993)
Eli Lilly
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
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
Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT.
J Med Chem 36: 221-8 (1993)
University Of Pennsylvania
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
o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents.
J Med Chem 36: 157-61 (1993)
Università
Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor.
Mol Pharmacol 46: 227-34 (1994)
Eli Lilly
8-Azaxanthine derivatives as antagonists of adenosine receptors.
J Med Chem 37: 2970-5 (1994)
Università
Synthesis and structure-activity relationships of novel retinoid X receptor-selective retinoids.
J Med Chem 37: 2930-41 (1994)
Ligand Pharmaceuticals
Stereospecific synthesis of peptidyl alpha-keto amides as inhibitors of calpain.
J Med Chem 37: 2918-29 (1994)
Alkermes
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
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
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
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
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
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
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
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
Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase.
J Med Chem 37: 2721-34 (1994)
Pfizer
Cyclic peptides with a phosphinic bond as potent inhibitors of a zinc bacterial collagenase.
J Med Chem 37: 2713-20 (1994)
University Of Athens
Substituted 1,3-dipropylxanthines as irreversible antagonists of A1 adenosine receptors.
J Med Chem 37: 2704-12 (1994)
University Of South Florida
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
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
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
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
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
SB-202742, a novel beta-lactamase inhibitor isolated from Spondias mombin.
J Nat Prod 57: 654-7 (1994)
Smithkline Beecham Pharmaceuticals
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
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
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
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
Structure-based design of inhibitors of purine nucleoside phosphorylase. 5. 9-Deazahypoxanthines.
J Med Chem 37: 2477-80 (1994)
Southern Research Institute
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
Leukotriene B4 (LTB4) receptor antagonists: a series of (hydroxyphenyl)pyrazoles.
J Med Chem 37: 2411-20 (1994)
Eli Lilly
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
Synthesis and SAR studies of novel triazolopyrimidine derivatives as potent, orally active angiotensin II receptor antagonists.
J Med Chem 37: 2371-86 (1994)
Carpibem
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
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
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
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
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
Crystal-structure-based design and synthesis of novel C-terminal inhibitors of HIV protease.
J Med Chem 37: 2274-84 (1994)
Agouron Pharmaceuticals
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
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
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
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
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
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
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
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
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
A new series of PDGF receptor tyrosine kinase inhibitors: 3-substituted quinoline derivatives.
J Med Chem 37: 2129-37 (1994)
RhôNe-Poulenc Rorer
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
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
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
Thienyl and thiazolyl acyclic analogues of 5-deazatetrahydrofolic acid.
J Med Chem 37: 2112-5 (1994)
Wellcome Research Laboratories
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
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
Selective inhibitors of monoamine oxidase. 2. Arylamide SAR.
J Med Chem 37: 2085-9 (1994)
Burroughs Wellcome
Novel acyl-CoA:cholesterol acyltransferase inhibitors. Synthesis and biological activity of 3-quinolylurea derivatives.
J Med Chem 37: 2079-84 (1994)
Takeda Chemical Industries
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
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
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
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
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
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
Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.
J Med Chem 37: 1996-2000 (1994)
Pfizer
Synthesis and characterization of selective fluorescent ligands for the neurokinin NK2 receptor.
J Med Chem 37: 1991-5 (1994)
Glaxo Institute For Molecular Biology
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
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
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
(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
(R)-methanandamide: a chiral novel anandamide possessing higher potency and metabolic stability.
J Med Chem 37: 1889-93 (1994)
University Of Connecticut
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
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
A new series of photoactivatable and iodinatable linear vasopressin antagonists.
J Med Chem 37: 1841-9 (1994)
Upr 9023 Cnrs
Dual angiotensin converting enzyme/thromboxane synthase inhibitors.
J Med Chem 37: 1823-32 (1994)
Ciba-Geigy
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
Three-dimensional pharmacophores from binding data.
J Med Chem 37: 1769-78 (1994)
Ciba-Geigy
Aminodiol HIV protease inhibitors. 1. Design, synthesis, and preliminary SAR.
J Med Chem 37: 1758-68 (1994)
Bristol-Myers Squibb
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
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
2-Azetidinones as inhibitors of cholesterol absorption.
J Med Chem 37: 1733-6 (1994)
Schering-Plough Research Institute
Curated by BindingDB
Curated by ChEMBL