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