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Hybromet: a ligand for purifying opioid receptors.
J Med Chem 28: 1950-3 (1986)
TBA
3-Phenyl-1-indanamines. Potential antidepressant activity and potent inhibition of dopamine, norepinephrine, and serotonin uptake.
J Med Chem 28: 1817-28 (1986)
TBA
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers.
J Med Chem 28: 1766-71 (1986)
TBA
N-(1,3,4,6,7,12b-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin -2-yl)-N- methyl-2-hydroxyethane-sulfonamide: a potent and selective alpha 2-adrenoceptor antagonist.
J Med Chem 28: 1756-9 (1986)
TBA
Novel nonnarcotic analgesics with an improved therapeutic ratio. Structure-activity relationships of 8-(methylthio)- and 8-(acylthio)-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines.
J Med Chem 28: 1656-61 (1985)
TBA
Structure-activity relationships among benextramine-related tetraamine disulfides at peripheral alpha-adrenoreceptors.
J Med Chem 28: 1643-7 (1985)
TBA
GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol.
J Med Chem 28: 1612-7 (1985)
TBA
Angiotensin converting enzyme inhibitors: N-substituted D-glutamic acid gamma dipeptides.
J Med Chem 28: 1606-11 (1985)
TBA
Angiotensin converting enzyme inhibitors: structure-activity profile of 1-benzazepin-2-one derivatives.
J Med Chem 28: 1603-6 (1985)
TBA
Xanthine derivatives as antagonists at A1 and A2 adenosine receptors.
Naunyn Schmiedebergs Arch Pharmacol 330: 212-21 (1985)
TBA
Angiotensin converting enzyme inhibitors: 1,5-benzothiazepine derivatives.
J Med Chem 28: 1517-21 (1985)
TBA
Synthesis and biological properties of (carboxyalkyl)amino-substituted bicyclic lactam inhibitors of angiotensin converting enzyme.
J Med Chem 28: 1511-6 (1985)
TBA
Synthesis and activity of 5-(aminomethylene)-1,3-cyclohexanediones: enolic analogues of gamma-aminobutyric acid.
J Med Chem 28: 1440-6 (1985)
TBA
N alpha-(diphenoxyphosphoryl)-L-alanyl-L-proline, N alpha-[bis (4-nitrophenoxy)phosphoryl]-L-alanyl-L-proline, and N alpha-[ (2-phenylethyl)phenoxyphosphoryl]-L-alanyl-L-proline: releasers of potent inhibitors of angiotensin converting enzyme at physiological pH and temperature.
J Med Chem 28: 1422-7 (1985)
TBA
N6-cycloalkyladenosines. Potent, A1-selective adenosine agonists.
J Med Chem 28: 1383-4 (1985)
TBA
Replacement of the ribofuranose oxygen of 2-5A derivatives by methylene: synthesis of an aristeromycin analogue of 2-5A core 5'-monophosphate (5'-O-phosphoryladenylyl)(2'----5')adenyl(2'----5')adenosine.
J Med Chem 28: 1376-80 (1985)
TBA
Functionalized congeners of adenosine: preparation of analogues with high affinity for A1-adenosine receptors.
J Med Chem 28: 1341-6 (1985)
TBA
Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors.
J Med Chem 28: 1334-40 (1985)
TBA
Quantitative evaluation of the beta 2-adrenoceptor affinity of phenoxypropanolamines and phenylethanolamines.
J Med Chem 28: 1328-34 (1985)
TBA
Synthesis and biological activity of modified peptide inhibitors of angiotensin-converting enzyme.
J Med Chem 28: 1291-5 (1985)
TBA
Synthesis and biological evaluation of phosphonamidate peptide inhibitors of enkephalinase and angiotensin-converting enzyme.
J Med Chem 28: 1208-16 (1985)
TBA
Synthesis and pharmacological characterization of 5-(2-dodecylphenyl)-4,6-dithianonanedioic acid and 5-[2-(8-phenyloctyl)phenyl]-4,6-dithianonanedioic acid: prototypes of a novel class of leukotriene antagonists.
J Med Chem 28: 1145-7 (1985)
TBA
Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.
J Med Chem 28: 1071-9 (1985)
TBA
Displacement of DL-[3H]-2-amino-4-phosphonobutanoic acid ( [3H]APB) binding with methyl-substituted APB analogues and glutamate agonists.
Biochemistry 24: 2401-5 (1985)
University Of Minnesota
Synthesis, in vitro [3H]prazosin displacement, and in vivo activity of 3-aryl-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridines, a new class of antihypertensive agents.
J Med Chem 28: 934-40 (1985)
TBA
Synthesis and biological activities of 2-pyrimidinone nucleosides. 2. 5-Halo-2-pyrimidinone 2'-deoxyribonucleosides.
J Med Chem 28: 904-10 (1985)
TBA
Sigma opioid receptor: characterization and co-identity with the phencyclidine receptor.
J Pharmacol Exp Ther 233: 597-602 (1985)
Eli Lilly
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
J Med Chem 28: 653-60 (1985)
TBA
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.
J Med Chem 28: 537-45 (1985)
TBA
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
J Med Chem 28: 487-92 (1985)
TBA
Conformational analysis and active site modelling of angiotensin-converting enzyme inhibitors.
J Med Chem 28: 393-9 (1985)
TBA
Angiotensin converting enzyme inhibitors. (Mercaptoaroyl)amino acids.
J Med Chem 28: 328-32 (1985)
TBA
N-[2-hydroxy-5-[2-(methylamino)ethyl]phenyl]methanesulfonamide. A potent agonist which releases intracellular calcium by activation of alpha 1-adrenoceptors.
J Med Chem 28: 245-8 (1985)
TBA
Angiotensin-converting enzyme inhibitors. New orally active antihypertensive (mercaptoalkanoyl)- and [(acylthio)alkanoyl]glycine derivatives.
J Med Chem 28: 57-66 (1985)
TBA
[3H]SCH 23390 labels both dopamine-1 and 5-hydroxytryptamine1c receptors in the choroid plexus.
J Pharmacol Exp Ther 247: 343-8 (1988)
University Of Pennsylvania
Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (+/-)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1] hept-2-exo-yl]heptenoic acid.
J Med Chem 31: 1847-54 (1988)
Shionogi
Synthesis and evaluation of multisubstrate inhibitors of an oncogene-encoded tyrosine-specific protein kinase. 1.
J Med Chem 31: 1762-7 (1988)
Smith Kline & French Laboratories
Quantitative autoradiography of serotonin uptake sites in rat brain using [3H]cyanoimipramine.
Brain Res 454: 78-88 (1988)
Veterans Administration Medical Center
Preparation of 7-oxaaporphine derivatives and evaluation of their dopaminergic activity.
J Med Chem 31: 1466-71 (1988)
Cns Line
Characterization of [5,6-3H]SQ 29,548 as a high affinity radioligand, binding to thromboxane A2/prostaglandin H2-receptors in human platelets.
J Pharmacol Exp Ther 245: 786-92 (1988)
Squibb Institute For Medical Research
Central dopaminergic and 5-hydroxytryptaminergic effects of C3-methylated derivatives of 8-hydroxy-2-(di-n-propylamino)tetralin.
J Med Chem 31: 1130-40 (1988)
University Of Uppsala
Dopamine D-2 receptor imaging radiopharmaceuticals: synthesis, radiolabeling, and in vitro binding of (R)-(+)- and (S)-(-)-3-iodo-2-hydroxy-6-methoxy-N- [(1-ethyl-2-pyrrolidinyl)methyl]benzamide.
J Med Chem 31: 1039-43 (1988)
University Of Pennsylvania
N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin.
J Med Chem 31: 867-70 (1988)
Virginia Commonwealth University
Design, synthesis, and biological activity of a peptide mimic of vasopressin.
J Med Chem 31: 742-4 (1988)
Smith Kline And French Laboratories
Potent vasopressin antagonists modified at the carboxy-terminal tripeptide tail.
J Med Chem 30: 2291-4 (1987)
Research And Development Division
Characterization of D-2 dopamine receptors in a tumor of the rat anterior pituitary gland.
J Pharmacol Exp Ther 242: 950-6 (1987)
University Of Pennsylvania
Synthesis and evaluation of non-catechol D-1 and D-2 dopamine receptor agonists: benzimidazol-2-one, benzoxazol-2-one, and the highly potent benzothiazol-2-one 7-ethylamines.
J Med Chem 30: 1166-76 (1987)
TBA
Potent antagonists of vasopressin antidiuretic activity that lack the beta,beta-cyclopentamethylene-beta-mercaptopropionic acid substitution at position 1.
J Med Chem 29: 2425-6 (1987)
TBA
Potent vasopressin antagonists lacking the proline residue at position 7.
J Med Chem 29: 984-8 (1986)
TBA
Synthesis and biological properties of chitin synthetase inhibitors resistant to cellular peptidases.
J Med Chem 29: 802-9 (1986)
TBA
A quantitative structure-activity relationship and molecular graphics analysis of hydrophobic effects in the interactions of inhibitors with alcohol dehydrogenase.
J Med Chem 29: 615-20 (1986)
TBA
Novel vasopressin analogues that help define a minimum effective antagonist pharmacophore.
J Med Chem 28: 1759-60 (1986)
TBA
The histamine H2 receptor agonist impromidine: synthesis and structure-activity considerations.
J Med Chem 28: 1414-22 (1985)
TBA
A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testis.
J Biol Chem 264: 4924-7 (1989)
Nagoya University School Of Medicine
Effects of steroid D-ring modification on suicide inactivation and competitive inhibition of aromatase by analogues of androsta-1,4-diene-3,17-dione.
J Med Chem 32: 651-8 (1989)
Washington University
Preparation and biodistribution of 1-[2-(3-[125I]iodo-4-aminophenyl)ethyl]-4-[3-(trifluoromethyl) phenyl]piperazine and 1-[2-(3-[125I]iodo-4-azidophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl] piperazine.
J Med Chem 32: 543-7 (1989)
University Of Pennsylvania
Synthesis of gastrin antagonists, analogues of the C-terminal tetrapeptide of gastrin, by introduction of a beta-homo residue.
J Med Chem 32: 522-8 (1989)
Centre De Pharmacologie-Endocrinologie (Montpellier, France)
The 2-desamino and 2-desamino-2-methyl analogues of aminopterin do not inhibit dihydrofolate reductase but are potently toxic to tumor cells in culture.
J Med Chem 32: 517-20 (1989)
Harvard Medical School
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 3. Synthesis and evaluation of (alkenyloxy)-, (alkynyloxy)-, and (aralkyloxy)methyl quaternarized 2-[(hydroxyimino)methyl]-1-alkylimidazolium halides as reactivators and therapy for soman intoxication.
J Med Chem 32: 504-16 (1989)
Sri International
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
J Med Chem 32: 493-503 (1989)
Sri International
Conformationally restricted and conformationally defined tyramine analogues as inhibitors of phenylethanolamine N-methyltransferase.
J Med Chem 32: 478-86 (1989)
University Of Kansas
Synthesis, tubulin binding, antineoplastic evaluation, and structure-activity relationship of oncodazole analogues.
J Med Chem 32: 409-17 (1989)
Smith Kline & French Laboratories
Cardiotonic agents. 1-Methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3 (2H)-isoquinolinones and related compounds. Synthesis and activity.
J Med Chem 32: 351-7 (1989)
Mitsui Toatsu Chemicals
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
J Med Chem 32: 289-97 (1989)
Tanabe Seiyaku
N6-bicycloalkyladenosines with unusually high potency and selectivity for the adenosine A1 receptor.
J Med Chem 32: 8-11 (1989)
Warner-Lambert
Platelet activating factor antagonists: synthesis and structure-activity studies of novel PAF analogues modified in the phosphorylcholine moiety.
J Med Chem 32: 56-64 (1989)
Takeda Chemical Industries
Prostaglandin photoaffinity probes: synthesis and biological activity of azide-substituted 16-phenoxy- and 17-phenyl-PGF2 alpha prostaglandins.
J Med Chem 32: 256-64 (1989)
University Of Kentucky
Interactions of thiol-containing androgens with human placental aromatase.
J Med Chem 32: 203-13 (1989)
University Of Washington
Synthesis and biological evaluation of a monocyclic, fully functional analogue of compactin.
J Med Chem 32: 197-202 (1989)
University Of California
Phenolic metabolites of clomiphene: [(E,Z)-2-[4-(1,2-diphenyl-2-chlorovinyl)phenoxy]ethyl]diethylamine. Preparation, electrophilicity, and effects in MCF 7 breast cancer cells.
J Med Chem 32: 192-7 (1989)
University Of Georgia
Flavones. 2. Synthesis and structure-activity relationship of flavodilol and its analogues, a novel class of antihypertensive agents with catecholamine depleting properties.
J Med Chem 32: 183-92 (1989)
Pennwalt
2,2-Difluoro-5-hexyne-1,4-diamine: a potent enzyme-activated inhibitor of ornithine decarboxylase.
J Med Chem 32: 170-3 (1989)
Merrell Dow Research Institute
Quinazoline antifolates inhibiting thymidylate synthase: synthesis of four oligo(L-gamma-glutamyl) conjugates of N10-propargyl-5,8-dideazafolic acid and their enzyme inhibition.
J Med Chem 32: 160-5 (1989)
Pedagogical University
Benzodiazepine gastrin and brain cholecystokinin receptor ligands: L-365,260.
J Med Chem 32: 13-6 (1989)
Merck Sharp & Dohme Research Laboratories
Pharmacological profile of SCH39166: a dopamine D1 selective benzonaphthazepine with potential antipsychotic activity.
J Pharmacol Exp Ther 247: 1093-102 (1988)
Schering-Plough
McN-5652: a highly potent inhibitor of serotonin uptake.
J Pharmacol Exp Ther 247: 1032-8 (1988)
Mcneil Pharmaceutical
Neuroleptic binding to human brain receptors: relation to clinical effects.
Ann N Y Acad Sci 537: 435-42 (1988)
Mayo Clinic
Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.
J Med Chem 31: 2247-56 (1989)
H. Lundbeck
Synthesis and pharmacology of trans-4-n-propyl-3,4,4a,10b-tetrahydro-2H,5H-1-benzopyrano[4,3-b ]-1,4-oxazin-7- and -9-ols: the significance of nitrogen pKa values for central dopamine receptor activation.
J Med Chem 31: 2178-82 (1988)
State University Of Groningen
Design and synthesis of somatostatin analogues with topographical properties that lead to highly potent and specific mu opioid receptor antagonists with greatly reduced binding at somatostatin receptors.
J Med Chem 31: 2170-7 (1988)
University Of Arizona
Serotonergic properties of spiroxatrine enantiomers.
J Med Chem 31: 1965-8 (1988)
University Of Arizona
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
J Med Chem 31: 1934-40 (1988)
Duphar Research Laboratories
Structure-activity relationships among benextramine-related tetraamine disulfides. Chain length effect on alpha-adrenoreceptor blocking activity.
J Med Chem 31: 1861-6 (1988)
University Of Camerino
Retro-inverso concept applied to the complete inhibitors of enkephalin-degrading enzymes.
J Med Chem 31: 1825-31 (1988)
Ua 498 Cnrs
Substituted benzamides with conformationally restricted side chains. 2. Indolizidine derivatives as central dopamine receptor antagonists.
J Med Chem 31: 1708-12 (1988)
Beecham Pharmaceuticals Research Division
Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines.
J Med Chem 31: 1621-5 (1988)
Warner-Lambert
Polycyclic aryl- and heteroarylpiperazinyl imides as 5-HT1A receptor ligands and potential anxiolytic agents: synthesis and structure-activity relationship studies.
J Med Chem 31: 1382-92 (1988)
Wyeth-Ayerst Research
Methotrexate analogues. 34. Replacement of the glutamate moiety in methotrexate and aminopterin by long-chain 2-aminoalkanedioic acids.
J Med Chem 31: 1338-44 (1988)
Harvard Medical School
Indoline analogues of idazoxan: potent alpha 2-antagonists and alpha 1-agonists.
J Med Chem 31: 944-8 (1988)
Reckitt And Colman
1,3-Diamino-6,7-dimethoxyisoquinoline derivatives as potential alpha 1-adrenoceptor antagonists.
J Med Chem 31: 1036-9 (1988)
Pfizer
2,4-Diamino-6,7-dimethoxyquinoline derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
J Med Chem 31: 1031-5 (1988)
Pfizer
Comparison of the pharmacological characteristics of [3H]raclopride and [3H]SCH 23390 binding to dopamine receptors in vivo in mouse brain.
Eur J Pharmacol 146: 113-20 (1988)
Novo Industri
Atypical antipsychotic agents: patterns of activity in a series of 3-substituted 2-pyridinyl-1-piperazine derivatives.
J Med Chem 31: 618-24 (1988)
Bristol-Myers
2,4-Diamino-6,7-dimethoxyquinazolines. 4. 2-[4-(substituted oxyethoxy) piperidino] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
J Med Chem 31: 516-20 (1988)
Pfizer
Characterization of alpha-2 adrenergic receptors in the OK cell, an opossum kidney cell line.
J Pharmacol Exp Ther 244: 571-8 (1988)
University Of Missouri
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.
J Med Chem 31: 454-61 (1988)
Warner-Lambert
Conformational analysis and structural comparisons of (1R,3S)-(+)- and (1S,3R)-(-)-tefludazine, (S)-(+)- and (R)-(-)-octoclothepin, and (+)-dexclamol in relation to dopamine receptor antagonism and amine-uptake inhibition.
J Med Chem 31: 306-12 (1988)
University Of Lund
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
J Med Chem 30: 2099-104 (1987)
Duphar Research Laboratories
Design and synthesis of phosphonate inhibitors of glutamine synthetase.
J Med Chem 30: 2062-7 (1987)
Pennsylvania State University
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.
J Med Chem 30: 1906-10 (1987)
Istituto Superiore Di Sanit£
Antipsychotic activity of substituted gamma-carbolines.
J Med Chem 30: 1818-23 (1987)
Wyeth Laboratories
1,3-Dialkyl-4-(iminoarylmethyl)-1H-pyrazol-5-ols. A series of novel potential antipsychotic agents.
J Med Chem 30: 1807-12 (1987)
Warner-Lambert/Parke-Davis Pharmaceutical Research
2,4-Diamino-6,7-dimethoxyquinazolines. 3. 2-(4-Heterocyclylpiperazin-1-yl) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
J Med Chem 30: 1794-8 (1987)
Pfizer
N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity.
J Med Chem 30: 1709-11 (1987)
Parke-Davis Pharmaceutical Research Division
Charged analogues of chlorpromazine as dopamine antagonists.
J Med Chem 30: 1631-5 (1987)
TBA
Carbostyril derivatives having potent beta-adrenergic agonist properties.
J Med Chem 30: 1563-6 (1987)
TBA
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.
J Med Chem 30: 1555-62 (1987)
TBA
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.
J Med Chem 30: 1538-42 (1987)
TBA
Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.
J Med Chem 30: 1229-39 (1987)
TBA
Alpha-1 adrenergic receptor binding in aortas from rat and dog: comparison of [3H]prazosin and beta-iodo-[125I]-4-hydroxyphenyl-ethyl-aminomethyl-tetralone.
J Pharmacol Exp Ther 241: 875-81 (1987)
Unwersity Of Misscuri
Pharmacological evidence for alpha-2 adrenoceptor heterogeneity: differential binding properties of [3H]rauwolscine and [3H]idazoxan in rat brain.
J Pharmacol Exp Ther 241: 1092-8 (1987)
University Of California
2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
J Med Chem 30: 999-1003 (1987)
TBA
Psychotropic agents: synthesis and antipsychotic activity of substituted beta-carbolines.
J Med Chem 30: 1100-5 (1987)
TBA
Conformationally defined adrenergic agents. 5. Resolution, absolute configuration, and pharmacological characterization of the enantiomers of 2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline: a potent agonist at alpha-adrenoceptors.
J Med Chem 30: 1011-7 (1987)
TBA
Synthesis and neuroleptic activity of a series of 1-[1-(benzo-1,4-dioxan-2-ylmethyl)-4-piperidinyl]benzim idazolone derivatives.
J Med Chem 30: 814-9 (1987)
TBA
Flavones. 1. Synthesis and antihypertensive activity of (3-phenylflavonoxy)propanolamines without beta-adrenoceptor antagonism.
J Med Chem 30: 788-92 (1987)
TBA
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
J Med Chem 30: 612-5 (1987)
TBA
2,4-diamino-6,7-dimethoxyquinazolines. 1. 2-[4-(1,4-benzodioxan-2-ylcarbonyl)piperazin-1-yl] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
J Med Chem 30: 49-57 (1987)
TBA
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
J Med Chem 30: 185-93 (1987)
TBA
Conformationally defined adrenergic agents. 4. 1-(aminomethyl)phthalans: synthesis and pharmacological consequences of the phthalan ring oxygen atom.
J Med Chem 30: 178-84 (1987)
TBA
Peptides as receptor selectivity modulators of opiate pharmacophores.
J Med Chem 29: 1222-5 (1987)
TBA
Two stereoisomeric imidazoline derivatives: synthesis and optical and alpha 2-adrenoceptor activities.
J Med Chem 29: 1183-8 (1986)
TBA
Synthesis of 2-(4-substituted-1-piperazinyl)benzimidazoles as H1-antihistaminic agents.
J Med Chem 29: 1178-83 (1987)
TBA
6,7-Dichloro-1-(3,4,5-trimethoxybenzyl)-1,2,3,4-tetrahydroisoquinoline . A structurally novel beta-adrenergic receptor blocking agent.
J Med Chem 29: 2381-4 (1986)
TBA
Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.
J Med Chem 29: 2370-5 (1986)
TBA
Synthesis and antiallergic activity of a novel series of 5-lipoxygenase inhibitors.
J Med Chem 29: 2329-34 (1986)
TBA
1,3-Di(2-[5-3H]tolyl)guanidine: a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs.
Proc Natl Acad Sci U S A 83: 8784-8 (1986)
The Oregon Health Sciences University
Further validation of in vivo and in vitro pharmacological procedures for assessing the alpha 2/alpha 1-selectivity of test compounds: (1). Alpha-adrenoceptor antagonists.
Eur J Pharmacol 129: 49-55 (1986)
Janssen Pharmaceutica
Neuroleptics from the 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 3. Carboxamidoalkyl derivatives.
J Med Chem 29: 2108-11 (1986)
TBA
Neuroleptics from the 4a,9b-cis- and 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 2.
J Med Chem 29: 2093-9 (1986)
TBA
Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.
J Med Chem 29: 2000-3 (1986)
TBA
Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties.
J Med Chem 29: 1913-7 (1986)
TBA
Thiazole-4-carboxamide adenine dinucleotide (TAD). Analogues stable to phosphodiesterase hydrolysis.
J Med Chem 29: 1726-31 (1986)
TBA
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
J Med Chem 29: 1628-37 (1986)
TBA
Buspirone analogues. 2. Structure-activity relationships of aromatic imide derivatives.
J Med Chem 29: 1476-82 (1986)
TBA
Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2.
J Med Chem 29: 889-94 (1986)
TBA
Characterization of flufylline, fluprofylline, ritanserin, butanserin and R 56413 with respect to in-vivo alpha 1-,alpha 2- and 5-HT2-receptor antagonism and in-vitro affinity for alpha 1-,alpha 2- and 5-HT2-receptors: comparison with ketanserin.
J Pharm Pharmacol 38: 374-9 (1986)
TBA
Methotrexate analogues. 26. Inhibition of dihydrofolate reductase and folylpolyglutamate synthetase activity and in vitro tumor cell growth by methotrexate and aminopterin analogues containing a basic amino acid side chain.
J Med Chem 29: 655-60 (1986)
TBA
(1-Amino-2-propenyl) phosphonic acid, an inhibitor of alanine racemase and D-alanine:D-alanine ligase.
J Med Chem 29: 579-81 (1986)
TBA
Quantitative evaluation of the beta 2-adrenoceptor intrinsic activity of N-tert-butylphenylethanolamines.
J Med Chem 29: 549-54 (1986)
TBA
Conformationally defined adrenergic agents. 2. Catechol imidazoline derivatives: biological effects at alpha 1 and alpha 2 adrenergic receptors.
J Med Chem 29: 463-7 (1986)
TBA
Effects of remoxipride and some related new substituted salicylamides on rat brain receptors.
Acta Pharmacol Toxicol (Copenh) 58: 61-70 (1986)
Astra LÄKemedel
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
J Med Chem 29: 359-69 (1986)
TBA
Selective alpha-2 adrenoceptor blockade by SK&F 86466: in vitro characterization of receptor selectivity.
J Pharmacol Exp Ther 236: 90-6 (1986)
Smith Kline & French Laboratories
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
J Med Chem 28: 1811-7 (1985)
TBA
Alkylating beta-blockers: activity of isomeric bromoacetyl alprenolol menthanes.
J Med Chem 28: 1699-703 (1985)
TBA
Conformationally defined adrenergic agents. 1. Design and synthesis of novel alpha 2 selective adrenergic agents: electrostatic repulsion based conformational prototypes.
J Med Chem 28: 1398-404 (1985)
TBA
Acylmorphinans. A novel class of potent analgesic agents.
J Med Chem 28: 1177-80 (1985)
TBA
6,7-Dihydro-5-[[(cis-2-hydroxy-trans-3-phenoxycyclopentyl)amino] methyl]-2-methylbenzo[b]thiophen-4(5H)-one: a novel alpha 1-adrenergic receptor antagonist and renal vasodilator.
J Med Chem 28: 1142-5 (1985)
TBA
Synthesis and neuroleptic activity of 3-(1-substituted-4-piperidinyl)-1,2-benzisoxazoles.
J Med Chem 28: 761-9 (1985)
TBA
Conjugates of catecholamines. 5. Synthesis and beta-adrenergic activity of N-(aminoalkyl)norepinephrine derivatives.
J Med Chem 28: 634-42 (1985)
TBA
1-[3-(Diarylamino)propyl]piperidines and related compounds, potential antipsychotic agents with low cataleptogenic profiles.
J Med Chem 28: 606-12 (1985)
TBA
Characterization of the binding of [3H]-CGS 19755: a novel N-methyl-D-aspartate antagonist with nanomolar affinity in rat brain.
Br J Pharmacol 95: 932-8 (1988)
Ciba-Geigy
Highly potent and selective ligands for a new class H3 of histamine receptor.
Invest Radiol -2 (1988)
UnitÉ
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
J Med Chem 31: 2235-46 (1989)
Merck Sharp & Dohme Research Laboratories
Anticonvulsant activities of phenyl-substituted bicyclic 2,4-oxazolidinediones and monocyclic models. Comparison with binding to the neuronal voltage-dependent sodium channel.
J Med Chem 31: 2218-21 (1988)
University Of Alabama
Inhibitors of cyclic AMP phosphodiesterase. 4. Synthesis and evaluation of potential prodrugs of lixazinone (N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro-2- oxoimidazo[2,1-b]quinazolin-7-yl)-oxy]butyramide, RS-82856).
J Med Chem 31: 2145-52 (1988)
Syntex Research
Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline.
J Med Chem 31: 2136-45 (1988)
Syntex Research
Radioiodinated benzodiazepines: agents for mapping glial tumors.
J Med Chem 31: 2081-6 (1988)
University Of Michigan Medical Center
Effects of addition of a 2-methyl group to ethyl nipecotates (beta-meperidines) on receptor affinities and opiate agonist/antagonist activities.
J Med Chem 31: 2015-21 (1988)
Sri International
Syntheses and adrenergic activities of ring-fluorinated epinephrines.
J Med Chem 31: 1972-7 (1988)
National Institute Of Diabetes
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.
J Med Chem 31: 1891-7 (1988)
Ua 498 Cnrs
Synthesis and antiviral evaluation of 6'-substituted aristeromycins: potential mechanism-based inhibitors of S-adenosylhomocysteine hydrolase.
J Med Chem 31: 1798-804 (1988)
Syntex Research
Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity.
J Med Chem 31: 1778-85 (1988)
Ortho Pharmaceutical
Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.
J Med Chem 31: 1694-7 (1988)
Sterling-Winthrop Research Institute
Biochemical and pharmacological characterization of L-659,989: an extremely potent, selective and competitive receptor antagonist of platelet-activating factor.
J Pharmacol Exp Ther 246: 534-41 (1988)
Merck Sharp & Dohme Research Laboratories
2-(2-Aryl-2-oxoethylidene)-1,2,3,4-tetrahydropyridines. Novel isomers of 1,4-dihydropyridine calcium channel blockers.
J Med Chem 31: 1659-64 (1988)
Warner-Lambert
Synthesis, pharmacological action, and receptor binding affinity of the enantiomeric 1-(1-phenyl-3-methylcyclohexyl)piperidines.
J Med Chem 31: 1625-8 (1988)
National Institute Of Diabetes
N2-phenyldeoxyguanosine: a novel selective inhibitor of herpes simplex thymidine kinase.
J Med Chem 31: 1496-500 (1988)
Istituto Di Genetica Biochimica Ed Evoluzionistica
Dimeric 1,4-dihydropyridines as calcium channel antagonists.
J Med Chem 31: 1489-92 (1988)
State University Of New York
Dinucleotide analogues as inhibitors of thymidine kinase, thymidylate kinase, and ribonucleotide reductase.
J Med Chem 31: 1305-8 (1988)
Institute Of Cancer Research
Substituted 2-[(2-benzimidazolylsulfinyl)methyl]anilines as potential inhibitors of H+/K+ ATPase.
J Med Chem 31: 1215-20 (1988)
Searle Research And Development
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
J Med Chem 31: 1148-60 (1988)
Squibb Institute For Medical Research
(+/-)-4-tert-butyl-3-cyano-1-(4-ethynylphenyl)-2,6,7-trioxabi cyclo[2.2.2]octane: synthesis of a remarkably potent GABAA receptor antagonist.
J Med Chem 31: 1064-6 (1988)
University Of California
Synthesis and pharmacological activity of angiotensin converting enzyme inhibitors: N-(mercaptoacyl)-4-substituted-(S)-prolines.
J Med Chem 31: 875-85 (1988)
Schering-Plough
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
J Med Chem 31: 836-41 (1988)
University Of Minnesota
Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.
J Med Chem 31: 831-6 (1988)
Parke-Davis Research Unit
Chemistry and positive inotropic effect of pelrinone and related derivatives. A novel class of 2-methylpyrimidones as inotropic agents.
J Med Chem 31: 814-23 (1988)
Ayerst Laboratories Research
Structure-affinity relationships of arylquinolizines at alpha-adrenoceptors.
J Med Chem 31: 641-5 (1988)
Merck Sharp & Dohme Research Laboratories
Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines.
J Med Chem 31: 555-60 (1988)
Eli Lilly
Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides.
J Med Chem 31: 374-83 (1988)
University Of Paris
8-Cyclopentyl-1,3-dipropylxanthine (DPCPX)--a selective high affinity antagonist radioligand for A1 adenosine receptors.
Naunyn Schmiedebergs Arch Pharmacol 336: 204-10 (1987)
UniversitÄT Heidelberg
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
J Med Chem 30: 2283-6 (1987)
Kansas University
Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines.
J Med Chem 30: 2175-81 (1988)
University Of Lausanne
N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors.
J Med Chem 30: 2169-74 (1988)
University Of G£Teborg
Structure-activity relationships of cyclic opioid peptide analogues containing a phenylalanine residue in the 3-position.
J Med Chem 30: 2094-9 (1987)
Clinical Research Institute Of Montreal
Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.
J Med Chem 30: 1963-72 (1987)
Warner-Lambert
Cardiotonic agents. 7. Inhibition of separated forms of cyclic nucleotide phosphodiesterase from guinea pig cardiac muscle by 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones and related compounds. Structure-activity relationships and correlation with in vivo positive inotropic activi
J Med Chem 30: 1955-62 (1987)
Warner-Lambert
Synthesis of methotrexate-antibody conjugates by regiospecific coupling and assessment of drug and antitumor activities.
J Med Chem 32: 2426-31 (1989)
Dalhousie University
Potential antiatherosclerotic agents. 6. Hypocholesterolemic trisubstituted urea analogues.
J Med Chem 32: 2318-25 (1989)
American Cyanamid
(R)- and (S)-5,6,7,8-tetrahydro-1-hydroxy-N,N-dipropyl-9H-benzocyclohepten- 8-ylamine. Stereoselective interactions with 5-HT1A receptors in the brain.
J Med Chem 32: 2311-8 (1989)
University Of Uppsala
Linear and proximal benzo-separated alkylated xanthines as adenosine-receptor antagonists.
J Med Chem 32: 2247-54 (1989)
University Of South Florida
CGS 21680C, an A2 selective adenosine receptor agonist with preferential hypotensive activity.
J Pharmacol Exp Ther 251: 47-55 (1989)
Ciba-Geigy
Differentiation of 5-hydroxytryptamine2 receptor subtypes using 125I-R-(-)2,5-dimethoxy-4-iodo-phenylisopropylamine and 3H-ketanserin.
J Neurosci 9: 3482-90 (1989)
Stanford University
Synthesis and hypolipidemic and antidiabetogenic activities of beta,beta,beta',beta'-tetrasubstituted, long-chain dioic acids.
J Med Chem 32: 2072-84 (1989)
Hebrew University
Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist.
J Med Chem 32: 1057-62 (1989)
Johns Hopkins Medical Institutions
Approaches to isozyme-specific inhibitors. 16. A novel methyl-C5' covalent adduct of L-ethionine and beta,gamma-imido-ATP as a potent multisubstrate inhibitor of rat methionine adenosyltransferases.
J Med Chem 32: 885-90 (1989)
Fox Chase Cancer Center
Studies on semirigid tricyclic analogues of the nigrostriatal toxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine.
J Med Chem 32: 473-7 (1989)
University Of California
Quinones. 4. Novel eicosanoid antagonists: synthesis and pharmacological evaluation.
J Med Chem 32: 2214-21 (1989)
Takeda Chemical Industries
Squalene analogues containing isopropylidene mimics as potential inhibitors of pig liver squalene epoxidase and oxidosqualene cyclase.
J Med Chem 32: 2152-8 (1989)
State University Of New York
2-(Fluoromethyl)-3-phytyl-1,4-naphthoquinone and its 2,3-epoxide. Inhibition of vitamin K epoxide reductase.
J Med Chem 32: 2138-41 (1989)
Northwestern University
A potent, tissue-selective, synthetic inhibitor of HMG-CoA reductase.
J Med Chem 32: 2038-41 (1989)
Bristol Myers
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 13. Some alkenyl derivatives with high in vitro activity against anaerobic organisms.
J Med Chem 32: 1949-58 (1989)
Wellcome Research Laboratories
N-(phthalimidoalkyl) derivatives of serotonergic agents: a common interaction at 5-HT1A serotonin binding sites?
J Med Chem 32: 1921-6 (1989)
Virginia Commonwealth University
Sulfur-containing 1,3-dialkylxanthine derivatives as selective antagonists at A1-adenosine receptors.
J Med Chem 32: 1873-9 (1989)
Niddk
Pentadienyl carboxamide derivatives as antagonists of platelet-activating factor.
J Med Chem 32: 1820-35 (1989)
Roche Research Center
Biphenylcarboxamide derivatives as antagonists of platelet-activating factor.
J Med Chem 32: 1814-20 (1989)
Roche Research Center
9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics.
J Med Chem 32: 1805-13 (1989)
Hoechst-Roussel Pharmaceuticals
Tricyclic compounds as selective muscarinic receptor antagonists. 3. Structure-selectivity relationships in a series of cardioselective (M2) antimuscarinics.
J Med Chem 32: 1718-24 (1989)
Dr. Karl Thomae
Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted benzolactams.
J Med Chem 32: 1681-5 (1989)
Merck Sharp & Dohme Research Laboratories
C2,N6-disubstituted adenosines: synthesis and structure-activity relationships.
J Med Chem 32: 1667-73 (1989)
Warner-Lambert
Characterization of muscarinic receptors in human, guinea pig and rat lung.
J Pharmacol Exp Ther 250: 309-15 (1989)
UniversitÉ
Tetrahydrothiadiazoloisoquinolines: synthesis and inhibition of phenylethanolamine-N-methyltransferase.
J Med Chem 32: 1566-71 (1989)
Smith Kline & French Laboratories
Inhibition of mammalian folylpolyglutamate synthetase and human dihydrofolate reductase by 5,8-dideaza analogues of folic acid and aminopterin bearing a terminal L-ornithine.
J Med Chem 32: 1559-65 (1989)
Medical University Of South Carolina
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.
J Med Chem 32: 1522-8 (1989)
Institute Of Research
New kelatorphan-related inhibitors of enkephalin metabolism: improved antinociceptive properties.
J Med Chem 32: 1497-503 (1989)
University Of Paris
Synthesis of a tritium-labeled indolidan analogue and its use as a radioligand for phosphodiesterase-inhibitor cardiotonic binding sites.
J Med Chem 32: 1476-80 (1989)
Eli Lilly
Oxidation of neplanocin A to the corresponding 3'-keto derivative by S-adenosylhomocysteine hydrolase.
J Med Chem 32: 1415-8 (1989)
University Of Kansas
Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives.
J Med Chem 32: 1265-72 (1989)
Sankyo
Acid-sensitive latent inhibitors for proteolytic enzymes: synthesis and characterization.
J Med Chem 32: 1253-9 (1989)
Amherst College
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
J Med Chem 32: 1231-7 (1989)
National Institutes Of Health
Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogues of trans-2-(4-phenylpiperidino)cyclohexanol (vesamicol).
J Med Chem 32: 1217-30 (1989)
University Of California
Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors.
J Med Chem 32: 1184-90 (1989)
University Of Paris
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
J Med Chem 32: 1164-72 (1989)
University Of Toledo
Pentagalloylglucose, A Xanthine Oxidase Inhibitor from a Paraguayan Crude Drug, "Molle-I" (Schinus terebinthifolius)
J Nat Prod 52: 210-211 (1989)
TBA
A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260.
Eur J Pharmacol 162: 273-80 (1989)
Merck Sharp & Dohme Research Laboratories
Design and synthesis of inhibitors of N8-acetylspermidine deacetylase.
J Med Chem 32: 984-9 (1989)
University Of The Pacific
Synthesis and pharmacological evaluation of 4,4-disubstituted piperidines.
J Med Chem 32: 968-74 (1989)
Anaquest Pharmaceuticals
A multisubstrate adduct inhibitor of a purine biosynthetic enzyme with a picomolar dissociation constant.
J Med Chem 32: 937-40 (1989)
Pennsylvania State University
Electrophilic derivatives of purines as irreversible inhibitors of A1 adenosine receptors.
J Med Chem 32: 1043-51 (1989)
Niddk
Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
Mol Pharmacol 35: 469-76 (1989)
National Institute Of Mental Health
Topographic probes of angiotensin and receptor: potent angiotensin II agonist containing diphenylalanine and long-acting antagonists containing biphenylalanine and 2-indan amino acid in position 8.
J Med Chem 32: 898-903 (1989)
Washington State University
[(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors.
J Med Chem 32: 890-7 (1989)
Syntex Research
Conformationally restricted analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.
J Med Chem 32: 863-9 (1989)
University Of Uppsala
Quinazoline antifolates inhibiting thymidylate synthase: 2-desamino derivatives with enhanced solubility and potency.
J Med Chem 32: 847-52 (1989)
Institute Of Cancer Research
Synthesis of some novel potent and selective catechol O-methyltransferase inhibitors.
J Med Chem 32: 841-6 (1989)
Orion
Hybrid cholecystokinin (CCK) antagonists: new implications in the design and modification of CCK antagonists.
J Med Chem 32: 739-42 (1989)
Abbott Laboratories
Benzofurans as mechanism-based inhibitors of dopamine beta-hydroxylase.
J Med Chem 32: 735-7 (1989)
Pennsylvania State University
Is there a case for P-450 inhibitors in cancer treatment?
J Med Chem 32: 2231-9 (1989)
Janssen Research Foundation
2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 12. 1,2-Dihydroquinolylmethyl analogues with high activity and specificity for bacterial dihydrofolate reductase.
J Med Chem 32: 1942-9 (1989)
Wellcome Research Laboratories
Synthesis and receptor affinities of some conformationally restricted analogues of the dopamine D1 selective ligand (5R)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl- 1H-3-benzazepin-7-ol.
J Med Chem 32: 1913-21 (1989)
Schering-Plough
Detection of a novel serotonin receptor subtype (5-HT1E) in human brain: interaction with a GTP-binding protein.
J Neurochem 53: 465-71 (1989)
Albany Medical College
Renin inhibitors. Synthesis of transition-state analogue inhibitors containing phosphorus acid derivatives at the scissile bond.
J Med Chem 32: 1652-61 (1989)
Ciba-Geigy Pharmaceuticals Division
Azido glycols: potent, low molecular weight renin inhibitors containing an unusual post scissile site residue.
J Med Chem 32: 1371-8 (1989)
Abbott Laboratories
Rational design of enzyme inhibitors: multisubstrate analogue inhibitors.
J Med Chem 32: 2-7 (1989)
University Of Utah
Dehydroquinate synthase: the use of substrate analogues to probe the late steps of the catalyzed reaction.
Biochemistry 28: 7572-82 (1989)
Harvard University
Microsomal delta 8,14-sterol delta 14-reductase in higher plants. Characterization and inhibition by analogues of a presumptive carbocationic intermediate of the reduction reaction.
Eur J Biochem 185: 605-14 (1989)
Institut De Botanique
Enkephalinase inhibitors. 1. 2,4-Dibenzylglutaric acid derivatives.
J Med Chem 32: 2519-26 (1989)
Ciba-Geigy
Thienothiopyran-2-sulfonamides: novel topically active carbonic anhydrase inhibitors for the treatment of glaucoma.
J Med Chem 32: 2510-3 (1989)
Merck Sharp And Dohme
Binding of arylpiperazines to 5-HT3 serotonin receptors: results of a structure-affinity study.
Eur J Pharmacol 168: 387-92 (1989)
Virginia Commonwealth University
Neurochemical profile of Lu 19-005, a potent inhibitor of uptake of dopamine, noradrenaline, and serotonin.
J Neurochem 44: 1615-22 (1985)
Lundbeck Ais
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
J Med Chem 28: 381-8 (1985)
TBA
Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics.
J Med Chem 32: 2573-82 (1989)
Eli Lilly
Substituted 5-amino-4,5,6,7-tetrahydroindazoles as partial ergoline structures with dopaminergic activity.
J Med Chem 32: 2388-96 (1989)
Eli Lilly
Synthesis and pharmacological evaluation of CNS activities of [1,2,3]triazolo[4,5-b][1,5]-, imidazolo[4,5-b][1,5]-, and pyrido[2,3-b][1,5]benzodiazepines. 10-Piperazinyl-4H-1,2,3-triazolo[4,5-b][1,5]benzodiazepines with neuroleptic activity.
J Med Chem 32: 2375-81 (1989)
Eli Lilly
Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties.
J Med Chem 32: 2273-6 (1989)
University Of G£Teborg
Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.
J Med Chem 32: 2261-8 (1989)
Vanderbilt University
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
J Med Chem 32: 2241-7 (1989)
Lusofarmaco
(8a alpha,12a alpha,13a alpha)-5,8,8a,9,10,11,12,12a,13,13a-decahydro- 3-methoxy-12-(methylsulfonyl)-6H-isoquino[2,1-g][1,6]naphthyridi ne, a potent and highly selective alpha 2-adrenoceptor antagonist.
J Med Chem 32: 2034-6 (1989)
Syntex Research
5-HT1A-receptor antagonism: N-alkyl derivatives of (R)-(-)-8,11-dimethoxynoraporphine.
J Med Chem 32: 1959-62 (1989)
College Of Pharmacy University Of Iowa
Heteroaromatic analogues of the alpha 2-adrenoreceptor partial agonist clonidine.
J Med Chem 32: 1627-30 (1989)
Reckitt & Colman
Highly selective kappa-opioid analgesics. 2. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide derivatives.
J Med Chem 32: 1620-6 (1989)
Parke-Davis Research Unit
Inhibition of aminopeptidases by peptides containing ketomethylene and hydroxyethylene amide bond replacements.
J Med Chem 32: 1378-92 (1989)
University Of Wisconsin-Madison
Synthesis and dopaminergic activity of 2-substituted octahydrobenzo[f]quinolines.
J Med Chem 32: 961-8 (1989)
University Of California
Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.
J Med Chem 32: 1052-6 (1989)
Mcneil Pharmaceutical And Janssen Research Foundation Worldwide
Synthesis and structure-activity relationship of substituted tetrahydro- and hexahydro-1,2-benzisothiazol-3-one 1,1-dioxides and thiadiazinones: potential anxiolytic agents.
J Med Chem 32: 1024-33 (1989)
Wyeth-Ayerst Research
Identification of structural requirements for analogues of atrial natriuretic peptide (ANP) to discriminate between ANP receptor subtypes.
J Med Chem 32: 869-74 (1989)
G. D. Searle
New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties.
J Med Chem 32: 663-71 (1989)
Boc Technical Center
A new series of tricyclic (aryloximino)propanolamines displaying very high selective beta 2-blocking properties.
J Med Chem 32: 315-20 (1989)
Université
Synthesis and antiallergy activity of 4-(diarylhydroxymethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds.
J Med Chem 32: 105-18 (1989)
A.H. Robins
Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity.
J Med Chem 32: 2399-406 (1989)
Suntory Institute For Biomedical Research
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.
J Med Chem 32: 2344-52 (1989)
Hebrew University Of Jerusalem
Active reduced-size hexapeptide analogues of luteinizing hormone-releasing hormone.
J Med Chem 32: 2340-4 (1989)
Abbott Laboratories
Type I and type II GABAA-benzodiazepine receptors produced in transfected cells.
Science 245: 1389-92 (1989)
UniversitÄT Heidelberg
Benzofuro[2,3-c]pyridin-6-ols: synthesis, affinity for opioid-receptor subtypes, and antinociceptive activity.
J Med Chem 32: 2221-6 (1989)
Ciba-Geigy
Evaluation and synthesis of aminohydroxyisoxazoles and pyrazoles as potential glycine agonists.
J Med Chem 32: 2116-28 (1989)
Warner-Lambert
LH-RH antagonists: design and synthesis of a novel series of peptidomimetics.
J Med Chem 32: 2036-8 (1989)
Abbott Laboratories
Characterization of the striatal M2 muscarinic receptor mediating inhibition of cyclic AMP using selective antagonists: a comparison with the brainstem M2 receptor.
J Pharmacol Exp Ther 250: 565-72 (1989)
Abbott Laboratories
Identification of two serine residues involved in agonist activation of the beta-adrenergic receptor.
J Biol Chem 264: 13572-8 (1989)
Merck Sharp And Dohme Research Laboratories
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
J Med Chem 32: 1996-2002 (1989)
National Institute Of Digestive
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
J Med Chem 32: 1842-60 (1989)
Roche Research Center
Angiotensin converting enzyme inhibitors: spirapril and related compounds.
J Med Chem 32: 1600-6 (1989)
Schering-Plough
Sodium channel binding and anticonvulsant activities for the enantiomers of a bicyclic 2,4-oxazolidinedione and monocyclic models.
J Med Chem 32: 1577-80 (1989)
University Of Alabama
Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues.
J Med Chem 32: 1450-7 (1989)
Centre De Neurochimie Du Cnrs
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
J Med Chem 32: 1402-7 (1989)
Institut De Pharmacologie (Ua 589 Cnrs)
Probes for narcotic receptor mediated phenomena. 15. (3S,4S)-(+)-trans-3-methylfentanyl isothiocyanate, a potent site-directed acylating agent for the delta opioid receptors in vitro.
J Med Chem 32: 1392-8 (1989)
National Institutes Of Health
Folate analogues. 32. Synthesis and biological evaluation of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid and related compounds.
J Med Chem 32: 1284-9 (1989)
University Of South Alabama
Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides.
J Med Chem 32: 1259-65 (1989)
Ciba-Geigy
Phencyclidine-like effects of tetrahydroisoquinolines and related compounds.
J Med Chem 32: 1242-8 (1989)
G. D. Searle
Synthesis and structure-activity relationships of a novel class of 5-lipoxygenase inhibitors. 2-(Phenylmethyl)-4-hydroxy-3,5-dialkylbenzofurans: the development of L-656,224.
J Med Chem 32: 1190-7 (1989)
Merck Frosst Canada
The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity.
J Med Chem 32: 1147-56 (1989)
Bristol-Myers
7-[3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4-dihydro-8- propyl-2H-1-benzopyran-2-carboxylic acid: an orally active selective leukotriene B4 receptor antagonist.
J Med Chem 32: 1145-7 (1989)
G.D. Searle And
Analogues of atriopeptin(103-125)amide having high binding selectivity.
J Med Chem 32: 1094-8 (1989)
G.D. Searle And
Design and synthesis of propranolol analogues as serotonergic agents.
J Med Chem 32: 859-63 (1989)
Virginia Commonwealth University
Computer-assisted design and synthesis of novel aldose reductase inhibitors.
J Med Chem 32: 757-65 (1989)
Wyeth-Ayerst Research
1-(m-chlorophenyl)piperazine (mCPP) interactions with neurotransmitter receptors in the human brain.
Biol Psychiatry 25: 569-75 (1989)
Stanford University
2H-[1]benzopyrano[3,4-b]pyridines: synthesis and activity at central monoamine receptors.
J Med Chem 32: 720-7 (1989)
Ciba-Geigy
Dermorphin analogues carrying an increased positive net charge in their"message" domain display extremely high mu opioid receptor selectivity.
J Med Chem 32: 698-703 (1989)
Clinical Research Institute Of Montreal
Synthesis of highly mu and delta opioid receptor selective peptides containing a photoaffinity group.
J Med Chem 32: 638-43 (1989)
University Of Arizona
Pharmacological characterization of the M1 muscarinic receptors expressed in murine fibroblast B82 cells.
J Pharmacol Exp Ther 248: 661-70 (1989)
University Of Arizona
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
J Med Chem 32: 418-21 (1989)
University Of Innsbruck
Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for the treatment of congestive heart failure.
J Med Chem 32: 342-50 (1989)
Warner-Lambert
Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.
J Med Chem 32: 302-4 (1989)
Smith Kline And French Laboratories
Alkylating prazosin analogue: irreversible label for alpha 1-adrenoceptors.
J Med Chem 32: 96-100 (1989)
National Institute On Aging/Grc
Conformationally restricted analogues of atriopeptin(103-125)amide.
J Med Chem 32: 67-72 (1989)
G.D. Searle And
Cloning of the cDNA and gene for a human D2 dopamine receptor.
Proc Natl Acad Sci U S A 86: 9762-6 (1989)
Oregon Health Sciences University
[125]I-spectramide: a novel benzamide displaying potent and selective effects at the D2 dopamine receptor.
Life Sci 45: 1821-9 (1989)
Nida Addiction Research Center
Characterization of an 125I-labeled thromboxane A2/prostaglandin H2 receptor agonist.
J Pharmacol Exp Ther 251: 557-62 (1989)
Medical University Of South Carolina
The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action.
Eur J Pharmacol 166: 493-504 (1989)
Novo Industri
Conformational analysis and molecular modeling of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as D1 dopamine receptor ligands.
J Med Chem 32: 2050-8 (1989)
University Of North Carolina
(+/-)-7-chloro-8-hydroxy-1-(4'-[125I]iodophenyl)-3-methyl-2,3,4,5- tetrahydro-1H-3-benzazepine: a potential CNS D-1 dopamine receptor imaging agent.
J Med Chem 32: 1431-5 (1989)
University Of Pennsylvania
2-Haloaporphines as potent dopamine agonists.
J Med Chem 32: 1198-201 (1989)
Northeastern University
9,11-Epoxy-9-homo-14-thiaprost-5-enoic acid derivatives: potent thromboxane A2 antagonists.
J Med Chem 32: 974-84 (1989)
Squibb Institute For Medical Research
A minor modification of residue 1 in potent vasopressin antagonists dramatically reduces agonist activity.
J Med Chem 32: 880-4 (1989)
Smith Kline & French Laboratories
Synthesis and D2 dopaminergic activity of pyrrolidinium, tetrahydrothiophenium, and tetrahydrothiophene analogues of sulpiride.
J Med Chem 32: 874-80 (1989)
Ohio State University
Resolved N,N-dialkylated 2-amino-8-hydroxytetralins: stereoselective interactions with 5-HT1A receptors in the brain.
J Med Chem 32: 779-83 (1989)
University Of Uppsala
Carboxyalkyl dipeptides with atrial natriuretic factor potentiating and antihypertensive activity.
J Med Chem 32: 737-9 (1989)
Schering-Plough Research Institute
Structure-activity relationships of novel vasopressin antagonists containing C-terminal diaminoalkanes and (aminoalkyl)guanidines.
J Med Chem 32: 391-6 (1989)
Smith Kline & French Laboratories
2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites.
J Med Chem 32: 253-6 (1989)
Virginia Commonwealth University
Tetrapeptide inhibitors of the IgA1 proteinases from type I Neisseria gonorrhoeae.
J Med Chem 32: 2407-11 (1989)
University Hospital
Design of potential anti-HIV agents. 1. Mannosidase inhibitors.
J Med Chem 32: 2084-9 (1989)
Csiro Division Of Chemicals And Polymers
On the structure selectivity problem in drug design. A comparative study of benzylpyrimidine inhibition of vertebrate and bacterial dihydrofolate reductase via molecular graphics and quantitative structure-activity relationships.
J Med Chem 32: 1895-905 (1989)
Pomona College
Differential effects of a series of hydroxamic acid derivatives on 5-lipoxygenase and cyclooxygenase from neutrophils and 12-lipoxygenase from platelets and their in vivo effects on inflammation and anaphylaxis.
J Med Chem 32: 1836-42 (1989)
Rorer Central Research
Folate analogues. 31. Synthesis of the reduced derivatives of 11-deazahomofolic acid, 10-methyl-11-deazahomofolic acid, and their evaluation as inhibitors of glycinamide ribonucleotide formyltransferase.
J Med Chem 32: 1277-83 (1989)
University Of South Alabama
Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors.
J Med Chem 32: 1208-13 (1989)
Pfizer
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
J Med Chem 32: 1176-83 (1989)
Wyeth-Ayerst Research
Inhibition studies on the membrane-associated phospholipase A2 in vitro and prostaglandin E2 production in vivo of the macrophage-like P388D1 cell. Effects of manoalide, 7,7-dimethyl-5,8-eicosadienoic acid, and p-bromophenacyl bromide.
J Biol Chem 264: 8520-8 (1989)
University Of California San Diego
Synthesis and antiproliferative effects of novel 5'-fluorinated analogues of 5'-deoxy-5'-(methylthio)adenosine.
J Med Chem 32: 997-1001 (1989)
Institute
Antiinflammatory activity of a series of substituted 2,3-dihydro-6-hydroxypyrimido[2,1-f]purine-4,8(1H,9H)-diones.
J Med Chem 32: 1118-27 (1989)
Schering-Plough
Synthesis and in vitro aldose reductase inhibitory activity of compounds containing an N-acylglycine moiety.
J Med Chem 32: 1033-8 (1989)
Auburn University
Synthesis and activity of nonhydrolyzable pseudomonic acid analogues.
J Med Chem 32: 151-60 (1989)
Abbott Laboratories
N- and 2-substituted N-(phenylsulfonyl)glycines as inhibitors of rat lens aldose reductase.
J Med Chem 32: 145-51 (1989)
Auburn University
Antiinflammatory 2,6-di-tert-butyl-4-(2-arylethenyl)phenols.
J Med Chem 32: 100-4 (1989)
Boehringer Ingelheim Pharmaceuticals
A novel lead for specific anti-HIV-1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine.
J Med Chem 32: 2507-9 (1989)
Showa University
Synthesis and biological activity of some partially modified retro-inverso analogues of cholecystokinin.
J Med Chem 32: 2331-9 (1989)
Centre De Pharmacologie-Endocrinologie (Montpellier, France)
Opioid agonist and antagonist activities of peripherally selective derivatives of naltrexamine and oxymorphamine.
J Med Chem 32: 2068-71 (1989)
University Of Minnesota
Acrylamide derivatives as antiallergic agents. 2. Synthesis and structure-activity relationships of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acryl amides.
J Med Chem 32: 583-93 (1989)
Dainippon Pharmaceutical
Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue.
J Med Chem 32: 445-9 (1989)
University Of Paris
6-substituted 1,3,4,5-tetrahydrobenz[cd]indol-4-amines: potent serotonin agonists.
J Med Chem 31: 1746-53 (1988)
Eli Lilly
Synthesis and biological activity of CCK26-33-related analogues modified in position 31.
J Med Chem 31: 966-70 (1988)
University Of Paris
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.
J Med Chem 31: 181-5 (1988)
University Of South Alabama
Hybrid bivalent ligands with opiate and enkephalin pharmacophores.
J Med Chem 30: 1991-4 (1987)
University Of Minnesota
Binary drugs: conjugates of purines and a peptide that bind to both adenosine and substance P receptors.
J Med Chem 30: 1529-32 (1987)
TBA
Synthesis and biological activities of pseudopeptide analogues of the C-terminal heptapeptide of cholecystokinin. On the importance of the peptide bonds.
J Med Chem 30: 1366-73 (1987)
TBA
Investigation of peripheral cholecystokinin receptor heterogeneity by cyclic and related linear analogues of CCK26-33: synthesis and biological properties.
J Med Chem 30: 962-8 (1987)
TBA
Structural aspects of ryanodine action and selectivity.
J Med Chem 30: 710-6 (1987)
TBA
Diethyl 3,6-dihydro-2,4-dimethyl-2,6-methano-1,3-benzothiazocine-5,11- dicarboxylates as calcium entry antagonists: new conformationally restrained analogues of Hantzsch 1,4-dihydropyridines related to nitrendipine as probes for receptor-site conformation.
J Med Chem 30: 690-5 (1987)
TBA
Synthesis and biological activity of novel calcium channel blockers: 2,5-dihydro-4-methyl-2-phenyl-1,5-benzothiazepine-3-carboxylic acid esters and 2,5-dihydro-4-methyl-2-phenyl-1,5-benzodiazepine-3-carboxylic acid esters.
J Med Chem 30: 635-40 (1987)
TBA
[pGlu6,Pro9]SP6-11, a selective agonist for the substance P P-receptor subtype.
J Med Chem 29: 1284-8 (1987)
TBA
Antagonists of substance P. Further modifications of substance P antagonists obtained by replacing either positions 7, 9 or 7, 8 and 11 of SP with D-amino acid residues.
J Med Chem 29: 1171-8 (1987)
TBA
Methotrexate analogues. 29. Effect of gamma-aminobutyric acid spacers between the pteroyl and glutamate moieties on enzyme binding and cell growth inhibition.
J Med Chem 29: 1872-6 (1986)
TBA
Syntheses and antifolate activity of 5-methyl-5-deaza analogues of aminopterin, methotrexate, folic acid, and N10-methylfolic acid.
J Med Chem 29: 1080-7 (1986)
TBA
Characterization and autoradiographic localization of multiple tachykinin binding sites in gastrointestinal tract and bladder.
J Pharmacol Exp Ther 236: 819-31 (1986)
National Institutes Of Health
Arginine-vasopressin analogues with high antidiuretic/vasopressor selectivity. Synthesis, biological activity, and receptor binding affinity of arginine-vasopressin analogues with substitutions in positions 1, 2, 4, 7, and 8.
J Med Chem 29: 96-9 (1986)
TBA
A comparison between dopamine-stimulated adenylate cyclase and 3H-SCH 23390 binding in rat striatum.
Life Sci 37: 1971-83 (1985)
UniversitÉ
Opioid agonists and antagonists. 6-Desoxy-6-substituted lactone, epoxide, and glycidate ester derivatives of naltrexone and oxymorphone.
J Med Chem 28: 949-57 (1985)
TBA
Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites.
J Med Chem 33: 838-45 (1990)
Warner-Lambert
Aporphines as antagonists of dopamine D-1 receptors.
J Med Chem 33: 600-7 (1990)
Eli Lilly
Development of a high affinity and stereoselective photoaffinity label for the D-1 dopamine receptor: synthesis and resolution of 7-[125I]iodo-8-hydroxy-3-methyl-1-(4'-azidophenyl)-2,3,4,5-tetrahydro- 1H-3-benzazepine.
J Med Chem 33: 521-6 (1990)
Research Biochemicals
Renin inhibitors based on dipeptide analogues. Incorporation of the hydroxyethylene isostere at the P2/P3 sites.
J Med Chem 33: 371-4 (1990)
Abbott Laboratories
Crystallographic and molecular modeling studies on 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione and its butyl analogue, inhibitors of mammalian aromatase. Comparison with natural substrates: prediction of enantioselectivity for N-alkyl derivatives.
J Med Chem 33: 2673-9 (1990)
Institute Of Cancer Research
Dihydropyrimidine calcium channel blockers. 2. 3-substituted-4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines.
J Med Chem 33: 2629-35 (1990)
Squibb Institute For Medical Research
Approaches to isozyme-specific inhibitors. 17. Attachment of a selectivity-inducing substituent to a multisubstrate adduct. Implications for facilitated design of potent, isozyme-selective inhibitors.
J Med Chem 33: 2545-51 (1990)
Institute For Cancer Research
Inhibition of human leukocyte elastase. 3. Synthesis and activity of 3'-substituted cephalosporins.
J Med Chem 33: 2529-35 (1990)
Merck Sharp And Dohme Research Laboratories
Inhibition of human leukocyte elastase. 2. Inhibition by substituted cephalosporin esters and amides.
J Med Chem 33: 2522-8 (1990)
Merck Sharp And Dohme Research Laboratories
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.
J Med Chem 33: 2513-21 (1990)
Merck Sharp And Dohme Research Laboratories
7-Oxabicyclo[2.2.1]heptyl carboxylic acids as thromboxane A2 antagonists: aza omega-chain analogues.
J Med Chem 33: 2465-76 (1990)
Squibb Institute For Medical Research
Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis.
J Med Chem 33: 2452-5 (1990)
Institute Of Cancer Research
N-fluoroalkylated and N-alkylated analogues of the dopaminergic D-2 receptor antagonist raclopride.
J Med Chem 33: 2430-7 (1990)
Washington University
Trifluoromethylacetylenic alcohols as affinity labels: inactivation of estradiol dehydrogenase by a trifluoromethylacetylenic secostradiol.
J Med Chem 33: 2319-21 (1990)
Washington University
Binding of selective antagonists to four muscarinic receptors (M1 to M4) in rat forebrain.
Mol Pharmacol 38: 267-73 (1990)
UniversitÉ
4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants.
J Med Chem 33: 2240-54 (1990)
Pfizer
Synthesis, phencyclidine-like pharmacology, and antiischemic potential of meta-substituted 1-(1-phenylcyclohexyl)-1,2,3,6-tetrahydropyridines.
J Med Chem 33: 2211-5 (1990)
National Institute Of Diabetes
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
J Med Chem 33: 2108-13 (1990)
Istituto De Angeli
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
J Med Chem 33: 2087-93 (1990)
Pfizer
Potent inhibition of thymidylate synthase by two series of nonclassical quinazolines.
J Med Chem 33: 2045-51 (1990)
Warner-Lambert
Synthesis of 3-arylecgonine analogues as inhibitors of cocaine binding and dopamine uptake.
J Med Chem 33: 2024-7 (1990)
University Of Maryland
Inhibition of ornithine decarboxylase by the isomers of 1,4-dimethylputrescine.
J Med Chem 33: 1969-74 (1990)
Universidad De Buenos Aires
Conformational restriction of angiotensin II: cyclic analogues having high potency.
J Med Chem 33: 1935-40 (1990)
G.D. Searle And
5-Hydroxytryptamine (5-HT3) receptor antagonists. 1. Indazole and indolizine-3-carboxylic acid derivatives.
J Med Chem 33: 1924-9 (1990)
Beecham Pharmaceuticals Research Division
2-(Arylalkylamino)adenosin-5'-uronamides: a new class of highly selective adenosine A2 receptor ligands.
J Med Chem 33: 1919-24 (1990)
Ciba-Geigy
Novel piperidine derivatives. Synthesis and anti-acetylcholinesterase activity of 1-benzyl-4-[2-(N-benzoylamino)ethyl]piperidine derivatives.
J Med Chem 33: 1880-7 (1990)
Tsukuba Research Laboratories
1-(Thienylalkyl)imidazole-2(3H)-thiones as potent competitive inhibitors of dopamine beta-hydroxylase.
J Med Chem 33: 1866-73 (1990)
Merrell Dow Research Institute
Vinblastine and vincristine are inhibitors of monoamine oxidase B.
J Med Chem 33: 1845-8 (1990)
University Of Iowa
Syntheses and platelet aggregation inhibitory and antithrombotic properties of [2-[(omega-aminoalkoxy)phenyl]ethyl]benzenes.
J Med Chem 33: 1818-23 (1990)
Mitsubishi Kasei
Synthesis of quaternary amine ether lipids and evaluation of neoplastic cell growth inhibitory properties.
J Med Chem 33: 1812-8 (1990)
University Of North Carolina
Substituted vitamin K epoxide analogues. New competitive inhibitors and substrates of vitamin K1 epoxide reductase.
J Med Chem 33: 1790-7 (1990)
Northwestern University
Evolution of a series of peptidoleukotriene antagonists: synthesis and structure/activity relationships of 1,3,5-substituted indoles and indazoles.
J Med Chem 33: 1781-90 (1990)
Ici Pharmaceuticals Group
A model for the antagonist binding site on the adenosine A1 receptor, based on steric, electrostatic, and hydrophobic properties.
J Med Chem 33: 1708-13 (1990)
Center For Bio-Pharmaceutical Sciences
Inhibition of vertebrate squalene epoxidase by extended and truncated analogues of trisnorsqualene alcohol.
J Med Chem 33: 1698-701 (1990)
State University Of New York
Angiotensin-converting enzyme inhibitors. 9. Novel [[N-(1-carboxy-3-phenylpropyl)amino]acyl]glycine derivatives with diuretic activity.
J Med Chem 33: 1600-6 (1990)
Rorer Central Research
Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.
J Med Chem 33: 1594-600 (1990)
Merrell Dow Research Institute
[3H]TA-3090, a selective benzothiazepine-type calcium channel receptor antagonist: in vitro characterization.
J Pharmacol Exp Ther 253: 461-5 (1990)
Marion Merrell Dow
Dihydropyrimidine calcium channel blockers: 2-heterosubstituted 4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines.
J Med Chem 33: 1510-5 (1990)
Squibb Institute For Medical Research
Studies on hindered phenols and analogues. 2. 1,3-Benzoxathioles having SRS-A inhibiting activity.
J Med Chem 33: 1491-6 (1990)
Sankyo
Polyamine analogues with antitumor activity.
J Med Chem 33: 1369-75 (1990)
Merrell Dow Research Institute
Nonpeptide angiotensin II receptor antagonists: N-[(benzyloxy)benzyl]imidazoles and related compounds as potent antihypertensives.
J Med Chem 33: 1330-6 (1990)
E. I. Du Pont De Nemours And
The discovery of potent nonpeptide angiotensin II receptor antagonists: a new class of potent antihypertensives.
J Med Chem 33: 1312-29 (1990)
E. I. Du Pont De Nemours
Analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) in the treatment of experimental Pneumocystis carinii pneumonia.
J Med Chem 33: 1252-7 (1990)
University Of North Carolina
Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes.
J Med Chem 33: 1163-70 (1990)
Molecular Therapeutics
Synthesis and pharmacological studies of N-[4-[2-hydroxy-3-[[2-[4-(1H-imidazol-1- yl)phenoxy]ethyl]amino]propoxy]phenyl]methanesulfonamide, a novel antiarrhythmic agent with class II and class III activities.
J Med Chem 33: 1087-90 (1990)
Berlex Laboratories
Hydroxamic acid inhibitors of 5-lipoxygenase: quantitative structure-activity relationships.
J Med Chem 33: 992-8 (1990)
Abbott Laboratories
Small peptide inhibitors of smooth muscle myosin light chain kinase.
J Med Chem 33: 964-72 (1990)
Schering-Plough Research Institute
Inhibition of steroid 5 alpha-reductase by unsaturated 3-carboxysteroids.
J Med Chem 33: 943-50 (1990)
Smith Kline & French Laboratories
Steroidal A ring aryl carboxylic acids: a new class of steroid 5 alpha-reductase inhibitors.
J Med Chem 33: 937-42 (1990)
Smith Kline & French Laboratories
Selective inhibition of gamma-aminobutyric acid aminotransferase by (3R,4R),(3S,4S)- and (3R,4S),(3S,4R)-4-amino-5-fluoro-3-phenylpentanoic acids.
J Med Chem 33: 931-6 (1990)
Northwestern University
A structure-affinity study of the binding of 4-substituted analogues of 1-(2,5-dimethoxyphenyl)-2-aminopropane at 5-HT2 serotonin receptors.
J Med Chem 33: 1032-6 (1990)
Virginia Commonwealth University
Some benzyl-substituted imidazoles, triazoles, tetrazoles, pyridinethiones, and structural relatives as multisubstrate inhibitors of dopamine beta-hydroxylase. 4. Structure-activity relationships at the copper binding site.
J Med Chem 33: 781-9 (1990)
Smith Kline & French Laboratories
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 6. Trans-6-[2-(substituted-1-naphthyl)ethyl(or ethenyl)]-3,4,5,6-tetrahydro-4-hydroxy-2H-pyran-2-ones.
J Med Chem 33: 758-65 (1990)
Merck Sharp & Dohme Research Laboratories
5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin.
J Med Chem 33: 755-8 (1990)
Virginia Commonwealth University
Synthesis and antifolate properties of 10-alkyl-5,10-dideaza analogues of methotrexate and tetrahydrofolic acid.
J Med Chem 33: 673-7 (1990)
Sri International
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
J Med Chem 33: 646-52 (1990)
Wyeth Research
Novel glutamic acid derived cholecystokinin receptor ligands.
J Med Chem 33: 591-5 (1990)
Merck Sharp & Dohme Research Laboratories
Beta-lactam analogues of oxotremorine. 3- and 4-methyl-substituted 2-azetidinones.
J Med Chem 33: 580-4 (1990)
University Of Uppsala
Antitubulin effects of derivatives of 3-demethylthiocolchicine, methylthio ethers of natural colchicinoids, and thioketones derived from thiocolchicine. Comparison with colchicinoids.
J Med Chem 33: 567-71 (1990)
Niddk
Synthesis and biological activity of an acyclic analogue of 5,6,7,8-tetrahydrofolic acid, N-[4-[[3-(2,4-diamino-1,6-dihydro-6-oxo-5- pyrimidinyl)propyl]amino]-benzoyl]-L-glutamic acid.
J Med Chem 33: 561-7 (1990)
Wellcome Research Laboratories
Design and synthesis of 4H-3,1-benzoxazin-4-ones as potent alternate substrate inhibitors of human leukocyte elastase.
J Med Chem 33: 464-79 (1990)
Syntex Research
Synthesis and biological activity of new HMG-CoA reductase inhibitors. 1. Lactones of pyridine- and pyrimidine-substituted 3,5-dihydroxy-6-heptenoic (-heptanoic) acids.
J Med Chem 33: 52-60 (1990)
Hoechst
Estrogen synthetase inhibitors. 2. Comparison of the in vitro aromatase inhibitory activity for a variety of nitrogen heterocycles substituted with diarylmethane or diarylmethanol groups.
J Med Chem 33: 416-29 (1990)
Eli Lilly
Synthesis of peptidyl fluoromethyl ketones and peptidyl alpha-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and human neutrophil cathepsin G.
J Med Chem 33: 394-407 (1990)
Merrell Dow Research Institute
Inhibitors of cholesterol biosynthesis. 2. 1,3,5-trisubstituted [2-(tetrahydro-4-hydroxy-2-oxopyran-6-yl)ethyl]pyrazoles.
J Med Chem 33: 31-8 (1990)
Warner-Lambert
Synthesis of some 3-(1-azabicyclo[2.2.2]octyl) 3-amino-2-hydroxy-2-phenylpropionates: profile of antimuscarinic efficacy and selectivity.
J Med Chem 33: 307-10 (1990)
Nova Pharmaceutical
1-(substituted-benzyl)imidazole-2(3H)-thione inhibitors of dopamine beta-hydroxylase.
J Med Chem 33: 274-81 (1990)
University Of Illinois
Synthesis and antifolate properties of 9-alkyl-10-deazaminopterins.
J Med Chem 33: 212-5 (1990)
Sri International
Inhibitors of cholesterol biosynthesis. 1. trans-6-(2-pyrrol-1-ylethyl)-4-hydroxypyran-2-ones, a novel series of HMG-CoA reductase inhibitors. 1. Effects of structural modifications at the 2- and 5-positions of the pyrrole nucleus.
J Med Chem 33: 21-31 (1990)
Warner-Lambert
Inhibition of monoamine oxidases A and B by simple isoquinoline alkaloids: racemic and optically active 1,2,3,4-tetrahydro-, 3,4-dihydro-, and fully aromatic isoquinolines.
J Med Chem 33: 147-52 (1990)
University Of Texas
Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists.
J Med Chem 33: 13-6 (1990)
Pfizer
A novel, nonsteroidal inhibitor of androgen binding to the rat androgen binding protein: diethyl [[[3-(2,6-dimethyl-4-pyridinyl)-4-fluorophenyl]amino]methylene] propanedioate.
J Med Chem 33: 129-32 (1990)
Sterling Research Group
Alpha-diketone and alpha-keto ester derivatives of N-protected amino acids and peptides as novel inhibitors of cysteine and serine proteinases.
J Med Chem 33: 11-3 (1990)
Merrell Dow Research Institute
Synthesis and biochemical studies of 7-substituted 4,6-androstadiene-3,17-diones as aromatase inhibitors.
J Med Chem 33: 101-5 (1990)
Ohio State University
Chemical and biochemical studies of 2-propynylpyrrolidine derivatives. Restricted-rotation analogues of N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide (BM-5).
J Med Chem 33: 3190-8 (1990)
American Cyanamid
Resolved pyrrolidine, piperidine, and perhydroazepine analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.
J Med Chem 33: 3182-9 (1990)
Uppsala University
Synthesis and biochemical evaluation of tritium-labeled 1-methyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1H-indazole-3-carboxa mide, a useful radioligand for 5HT3 receptors.
J Med Chem 33: 3176-81 (1991)
Eli Lilly
A novel synthesis of xanthines: support for a new binding mode for xanthines with respect to adenosine at adenosine receptors.
J Med Chem 33: 3127-30 (1991)
Merrell Dow Research Institute
Characterization of muscarinic M4 binding sites in rabbit lung, chicken heart, and NG108-15 cells.
Mol Pharmacol 38: 805-15 (1990)
Glaxo Group Research
Quinazoline antifolate thymidylate synthase inhibitors: benzoyl ring modifications in the C2-methyl series.
J Med Chem 33: 3072-8 (1990)
Ici Pharmaceuticals Group
Quinazoline antifolate thymidylate synthase inhibitors: 2'-fluoro-N10-propargyl-5,8-dideazafolic acid and derivatives with modifications in the C2 position.
J Med Chem 33: 3067-71 (1990)
Institute Of Cancer Research
Quinazoline antifolate thymidylate synthase inhibitors: alkyl, substituted alkyl, and aryl substituents in the C2 position.
J Med Chem 33: 3060-7 (1990)
Ici Pharmaceuticals Group
Inhibition of enzymes of estrogen and androgen biosynthesis by esters of 4-pyridylacetic acid.
J Med Chem 33: 3050-5 (1990)
Institute Of Cancer Research
Synthesis, in vitro binding profile, and central nervous system penetrability of the highly potent 5-HT3 receptor antagonist [3H]-4-(2-methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole.
J Med Chem 33: 3020-3 (1990)
Pfizer
Synthesis, biological profile, and quantitative structure-activity relationship of a series of novel 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors.
J Med Chem 33: 2982-99 (1990)
Bristol-Myers Squibb
Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.
J Med Chem 33: 2956-61 (1990)
Abbott Laboratories
Mechanism and inhibition of cytochrome P-450 aromatase.
J Med Chem 33: 2933-42 (1990)
Johns Hopkins University School Of Medicine
7-Deaza-2-phenyladenines: structure-activity relationships of potent A1 selective adenosine receptor antagonists.
J Med Chem 33: 2822-8 (1990)
National Institute Of Diabetes
Imidazodiazepinediones: a new class of adenosine receptor antagonists.
J Med Chem 33: 2818-21 (1990)
National Institute Of Diabetes
Pyrroloisoquinoline antidepressants. 3. A focus on serotonin.
J Med Chem 33: 2793-7 (1990)
Mcneil Pharmaceutical
Binding of indolylalkylamines at 5-HT2 serotonin receptors: examination of a hydrophobic binding region.
J Med Chem 33: 2777-84 (1990)
Virginia Commonwealth University
Penta- and hexadienoic acid derivatives: a novel series of 5-lipoxygenase inhibitors.
J Med Chem 33: 2744-9 (1990)
Centre De Recherches De Vitry
Synthesis of acyclic and dehydroaspartic acid analogues of Ac-Asp-Glu-OH and their inhibition of rat brain N-acetylated alpha-linked acidic dipeptidase (NAALA dipeptidase).
J Med Chem 33: 2734-44 (1990)
University Of Minnesota
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.
J Med Chem 33: 2715-20 (1990)
Pfizer
Structure-based, C2 symmetric inhibitors of HIV protease.
J Med Chem 33: 2687-9 (1990)
Abbott Laboratories
Antiatherosclerotic agents. A structurally novel bivalent inhibitor of acylCoA:cholesterol O-acyltransferase with systemic activity.
J Med Chem 33: 2685-7 (1990)
Upjohn Laboratories
Biexponential kinetics of (R)-alpha-[3H]methylhistamine binding to the rat brain H3 histamine receptor.
J Neurochem 55: 1612-6 (1990)
Schering-Plough Research Institute
Inhibitors of human renin. Cyclic peptide analogues containing a D-Phe-Lys-D-Trp sequence.
J Med Chem 33: 2560-8 (1990)
Ici Pharmaceuticals Group
Novel inhibitors of human renin. Cyclic peptides based on the tetrapeptide sequence Glu-D-Phe-Lys-D-Trp.
J Med Chem 33: 2552-60 (1990)
Ici Pharmaceuticals Group
Alfred Burger award address. Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine.
J Med Chem 33: 2311-9 (1990)
Niddk
Design, activity, and 2.8 A crystal structure of a C2 symmetric inhibitor complexed to HIV-1 protease.
Science 249: 527-33 (1990)
Abbott Laboratories
Potent renin inhibitory peptides containing hydrophilic end groups.
J Med Chem 33: 2276-83 (1990)
Upjohn
Thermodynamics of the interaction of inhibitors with the binding site of recombinant human renin.
J Med Chem 33: 2080-6 (1990)
Upjohn
Water-soluble renin inhibitors: design of a subnanomolar inhibitor with a prolonged duration of action.
J Med Chem 33: 1962-9 (1990)
Abbott Laboratories
Muscarinic receptor subtypes.
Annu Rev Pharmacol Toxicol 30: 633-73 (1990)
National Institute For Medical Research
O'-(epoxyalkyl)tyrosines and (epoxyalkyl)phenylalanine as irreversible inactivators of serine proteases: synthesis and inhibition mechanism.
J Med Chem 33: 1620-34 (1990)
State University
Potent, low molecular weight renin inhibitors containing a C-terminal heterocycle: hydrogen bonding at the active site.
J Med Chem 33: 1582-90 (1990)
Abbott Laboratories
Renin inhibitory peptides. A beta-aspartyl residue as a replacement for the histidyl residue at the P-2 site.
J Med Chem 33: 1337-43 (1990)
Upjohn
Hydroxyethylamine analogues of the p17/p24 substrate cleavage site are tight-binding inhibitors of HIV protease.
J Med Chem 33: 1285-8 (1990)
University Of Wisconsin-Madison
Characterization of kappa 1 and kappa 2 opioid binding sites in frog (Rana esculenta) brain membrane preparation.
Neurochem Res 15: 899-904 (1990)
Biological Research Center Of Hungarian Academy Of Sciences
Thiazolidine-diones. Biochemical and biological activity of a novel class of tyrosine protein kinase inhibitors.
J Biol Chem 265: 22255-61 (1990)
Ciba-Geigy
4-Alkyl-1,4-dihydropyridines derivatives as specific PAF-acether antagonists.
J Med Chem 33: 3205-10 (1991)
Alter
Cloning, expression, and pharmacological characterization of a human alpha 2B-adrenergic receptor.
Mol Pharmacol 38: 681-8 (1990)
Neurogenetic
Amplification of the rat M2 muscarinic receptor gene by the polymerase chain reaction: functional expression of the M2 muscarinic receptor.
Life Sci 47: 1001-13 (1990)
University Of Arizona
Synthesis and evaluation of N-substituted cis-N-methyl-2-(1-pyrrolidinyl)cyclohexylamines as high affinity sigma receptor ligands. Identification of a new class of highly potent and selective sigma receptor probes.
J Med Chem 33: 3100-10 (1990)
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis and pharmacological evaluation of a series of new 3-methyl-1,4-disubstituted-piperidine analgesics.
J Med Chem 33: 2876-82 (1990)
Anaquest Pharmaceuticals
Propenyl carboxamide derivatives as antagonists of platelet activating factor.
J Med Chem 33: 2856-64 (1990)
Hoffmann-La Roche
Stereospecific synthesis, assignment of absolute configuration, and biological activity of the enantiomers of 3-[[[3-[2-(7-chloroquinolin-2-yl)-(E)-ethenyl]phenyl] [[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid, a potent and specific leukotriene D4 receptor antagonist.
J Med Chem 33: 2841-5 (1990)
Merck Frosst Centre For Therapeutic Research
The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.
J Med Chem 33: 2828-41 (1990)
Rorer Central Research
Benzophenone dicarboxylic acid antagonists of leukotriene B4. 2. Structure-activity relationships of the lipophilic side chain.
J Med Chem 33: 2807-13 (1990)
Eli Lilly
Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
J Med Chem 33: 2456-64 (1990)
Universit£
Receptor ligands which bind the oxytocin receptor with selectivity and high affinity. Chemical modification of a Streptomyces silvensis derived cyclic hexapeptide.
J Med Chem 33: 2321-3 (1990)
Merck
Electrophilic alpha-methylene-gamma-lactone and isothiocyanate opioid ligands related to etorphine.
J Med Chem 33: 2286-96 (1990)
University Of Washington
Purine derivatives as competitive inhibitors of human erythrocyte membrane phosphatidylinositol 4-kinase.
J Med Chem 33: 2073-80 (1990)
Smith Kline & French Research
Cyclic hexapeptide oxytocin antagonists. Potency-, selectivity-, and solubility-enhancing modifications.
J Med Chem 33: 1843-5 (1990)
Merck Sharp & Dohme Research Laboratories
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
J Med Chem 33: 1714-20 (1990)
University Of Minnesota
Angiotensin converting enzyme inhibitors. 10. Aryl sulfonamide substituted N-[1-carboxy-3-phenylpropyl]-L-alanyl-L-proline derivatives as novel antihypertensives.
J Med Chem 33: 1606-15 (1990)
Rorer Central Research
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity.
J Med Chem 33: 1194-200 (1990)
Rorer Central Research
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 1. Initial structure-activity relationships.
J Med Chem 33: 1186-94 (1990)
Rorer Central Research
Synthesis and alpha 2-adrenoceptor effects of substituted catecholimidazoline and catecholimidazole analogues in human platelets.
J Med Chem 33: 1138-44 (1990)
Ohio State University
Functional validation of platelet-activating factor receptor sites characterized biochemically by a specific and reproducible [3H]platelet-activating factor binding in human platelets.
J Pharmacol Exp Ther 252: 1221-7 (1990)
Rhone-Poulenc Sante
Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells.
J Biol Chem 265: 5267-72 (1990)
Nagoya University School Of Medicine
Synthesis and structure-activity relationship of C5-substituted analogues of (+-)-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine [(+-)-desmethyl-MK801]: ligands for the NMDA receptor-coupled phencyclidine binding site.
J Med Chem 33: 1069-76 (1990)
National Institute Of Diabetes And Digestive And Kidney Diseases
Functionalized congener approach for the design of novel muscarinic agents. Synthesis and pharmacological evaluation of N-methyl-N-[4-(1-pyrrolidinyl)-2-butynyl] amides.
J Med Chem 33: 741-8 (1990)
Niddk
Conjugate addition ligands of opioid antagonists. Methacrylate esters and ethers of 6 alpha- and 6 beta-naltrexol.
J Med Chem 33: 737-41 (1990)
University Of Washington
Synthesis and inhibitory potency of peptides corresponding to the subunit 2 C-terminal region of herpes virus ribonucleotide reductases.
J Med Chem 33: 723-30 (1990)
Notre-Dame Hospital Research
Synthesis and biological activity of atrial natriuretic factor analogues: effect of modifications to the disulfide bridge.
J Med Chem 33: 661-7 (1990)
Bio Mega Laboratories
1,9-Alkano-bridged 2,3,4,5-tetrahydro-1H-3-benzazepines with affinity for the alpha 2-adrenoceptor and the 5-HT1A receptor.
J Med Chem 33: 633-41 (1990)
Syntex Research
Affinity of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines for alpha-adrenoceptors. Differential affinity of imidazolines for the [3H]idazoxan-labeled alpha 2-adrenoceptor vs the [3H]yohimbine-labeled site.
J Med Chem 33: 596-600 (1990)
Syntex Research
Antiulcer agents. 4-substituted 2-guanidinothiazoles: reversible, competitive, and selective inhibitors of gastric H+,K(+)-ATPase.
J Med Chem 33: 543-52 (1990)
Pfizer
Reversible inhibitors of the gastric (H+/K+)-ATPase. 1. 1-Aryl-4-methylpyrrolo[3,2-c]quinolines as conformationally restrained analogues of 4-(arylamino)quinolines.
J Med Chem 33: 527-33 (1990)
Smith Kline & French Research
GABA agonists and uptake inhibitors. Synthesis, absolute stereochemistry, and enantioselectivity of (R)-(-)- and (S)-(+)-homo-beta-proline.
J Med Chem 33: 71-7 (1990)
Royal Danish School Of Pharmacy
Synthesis and biological activity of new HMG-CoA reductase inhibitors. 2. Derivatives of 7-(1H-pyrrol-3-yl)-substituted-3,5-dihydroxyhept-6(E)-enoic (-heptanoic) acids.
J Med Chem 33: 61-70 (1990)
Hoechst
Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.
J Med Chem 33: 450-5 (1990)
Merck Sharp & Dohme Research Laboratories
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
J Med Chem 33: 380-6 (1990)
R. W. Johnson Pharmaceutical Research Institute
Synthesis and cardiotonic activity of novel biimidazoles.
J Med Chem 33: 317-27 (1990)
Merrell Dow Research Institute
Highly selective kappa-opioid analgesics. 3. Synthesis and structure-activity relationships of novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted-cyclohexyl]arylacetamide derivatives.
J Med Chem 33: 286-91 (1990)
Parke-Davis Research Unit
Phosphoramidate peptide inhibitors of human skin fibroblast collagenase.
J Med Chem 33: 263-73 (1990)
University Of Kentucky
Synthesis and in vitro evaluation of some modified 4-thiopyrimidine nucleosides for prevention or reversal of AIDS-associated neurological disorders.
J Med Chem 33: 258-63 (1990)
Michigan Cancer Foundation
[D-Pen2,D-Pen5]enkephalin analogues with increased affinity and selectivity for delta opioid receptors.
J Med Chem 33: 249-53 (1990)
University Of Arizona
Assessment of the in vivo and in vitro opioid activity of bridged hexahydroaporphine and isoquinoline molecules.
J Med Chem 33: 245-8 (1990)
Creighton University
Structure-activity relationships of N2-substituted guanines as inhibitors of HSV1 and HSV2 thymidine kinases.
J Med Chem 33: 203-6 (1990)
University Of Massachusetts Medical School
Synthesis and dopamine receptor affinity of (R)-(-)-2-fluoro-N-n-propylnorapomorphine: a highly potent and selective dopamine D2 agonist.
J Med Chem 33: 3122-4 (1991)
Research Biochemicals
An initial three-component pharmacophore for specific serotonin-3 receptor ligands.
J Med Chem 33: 2721-5 (1990)
Pfizer
4-Isoxazolyl-1,4-dihydropyridines: biological, theoretical, and structural studies.
J Med Chem 33: 2255-9 (1990)
State University Of New York
(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist.
J Med Chem 33: 1541-4 (1990)
TBA
Characterization of D1 dopamine receptors in the bovine pineal gland with [3H]SCH 23390.
J Pharmacol Exp Ther 253: 214-20 (1990)
University Of Nebraska
Sodium-dependent isomerization of dopamine D-2 receptors characterized using [125I]epidepride, a high-affinity substituted benzamide ligand.
J Pharmacol Exp Ther 252: 1108-16 (1990)
Department Of Veterans Affairs Medical Center
Novel [(diazomethyl)carbonyl]-1,2,3,4-tetrahydronaphthalene derivatives as potential photoaffinity ligands for the 5-HT1A receptor.
J Med Chem 33: 950-5 (1990)
Mount Sinai School Of Medicine
Molecular cloning and expression of a dopamine D2 receptor from human retina.
Mol Pharmacol 37: 1-6 (1990)
National Institute Of Neurological Disorders And Stroke
New leupeptin analogues: synthesis and inhibition data.
J Med Chem 33: 86-93 (1990)
University Of Arkansas
Synthesis and structural requirements of N-substituted norapomorphines for affinity and activity at dopamine D-1, D-2, and agonist receptor sites in rat brain.
J Med Chem 33: 39-44 (1990)
Northeastern University
Synthesis and serotonin binding site studies of some conformationally restricted indolylethylamine analogues based on 2-amino-3-(3'-indolyl)bicyclo[2.2.2]octane.
J Med Chem 33: 386-94 (1990)
Polytechnic University
Synthesis and characterization of iodobenzamide analogues: potential D-2 dopamine receptor imaging agents.
J Med Chem 33: 171-8 (1990)
University Of Pennsylvania
Synthesis and pharmacology of the enantiomers of cis-7-hydroxy-3-methyl-2-(dipropylamino)tetralin.
J Med Chem 33: 2925-9 (1990)
Uppsala University
(Pyrimidinyloxy)acetic acids and pyrimidineacetic acids as a novel class of aldose reductase inhibitors.
J Med Chem 33: 2892-9 (1990)
Wyeth-Ayerst Research
Orally potent human renin inhibitors derived from angiotensinogen transition state: design, synthesis, and mode of interaction.
J Med Chem 33: 2707-14 (1990)
Kissei Pharmaceutical
Synthesis and quantitative structure-activity relationships of diclofenac analogues.
J Med Chem 33: 2358-68 (1990)
Ciba-Geigy
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 2. Synthesis, biological properties and molecular modeling of hydroxyethylene isostere derivatives.
J Med Chem 33: 2335-42 (1990)
Ici Pharmaceuticals Group
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 1. Synthesis and biological properties of alkyl alcohol and statine derivatives.
J Med Chem 33: 2326-34 (1990)
Ici Pharmaceuticals Group
Antiinflammatory agents. 4. Syntheses and biological evaluation of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid.
J Med Chem 33: 2296-304 (1990)
A.H. Robins
Nonsteroidal antiinflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase.
J Med Chem 33: 2070-2 (1990)
Warner-Lambert
1,2-Dihydro-1-oxopyrrolo[3,2,1-kl]phenothiazine-2-carboxamides and congeners, dual cyclooxygenase/5-lipoxygenase inhibitors with antiinflammatory activity.
J Med Chem 33: 2019-24 (1990)
Pfizer
Synthesis of (R)-(-)- and (S)-(+)-4-fluorodeprenyl and (R)-(-)- and (S)-(+)-[N-11C-methyl]-4-fluorodeprenyl and positron emission tomography studies in baboon brain.
J Med Chem 33: 2015-9 (1990)
Brookhaven National Laboratory
Effect of structure on potency and selectivity in 2,6-disubstituted 4-(2-arylethenyl)phenol lipoxygenase inhibitors.
J Med Chem 33: 1892-8 (1990)
Boehringer Ingelheim Pharmaceuticals
Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones.
J Med Chem 33: 1859-65 (1990)
Pfizer
New inhibitors of renin that contain novel phosphostatine Leu-Val replacements.
J Med Chem 33: 534-42 (1990)
Abbott Laboratories
2-substituted-1-naphthols as potent 5-lipoxygenase inhibitors with topical antiinflammatory activity.
J Med Chem 33: 360-70 (1990)
E.I. Du Pont De Nemours
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
J Med Chem 33: 240-5 (1990)
Wyeth-Ayerst Research
The main features of central 5-HT1 receptors.
Neuropsychopharmacology 3: 349-60 (1990)
Sorbonne University
Comparison of A1 adenosine receptors in brain from different species by radioligand binding and photoaffinity labelling.
Naunyn Schmiedebergs Arch Pharmacol 343: 196-201 (1991)
UniversitÄT Heidelberg
New pepstatin analogues: synthesis and pepsin inhibition.
J Med Chem 34: 2298-300 (1991)
University Of Arkansas
Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3- pyridine-carboxylate and analogues. Synthesis and structure-activity relationships.
J Med Chem 34: 2248-60 (1991)
Warner-Lambert
Purine and 1-deazapurine ribonucleosides and deoxyribonucleosides: synthesis and biological activity.
J Med Chem 34: 2226-30 (1991)
Universit£
Quinazoline antifolate thymidylate synthase inhibitors: bridge modifications and conformationally restricted analogues in the C2-methyl series.
J Med Chem 34: 2209-18 (1991)
Ici Pharmaceuticals Group
Syntheses of 5,7,8- and 5,6,7-trioxygenated 3-alkyl-3',4'-dihydroxyflavones and their inhibitory activities against arachidonate 5-lipoxygenase.
J Med Chem 34: 2169-76 (1991)
University Of Tokushima
4-hydroxythiazole inhibitors of 5-lipoxygenase.
J Med Chem 34: 2158-65 (1991)
Abbott Laboratories
Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine.
J Med Chem 34: 2133-45 (1991)
Niddk
Determination of dissociation constants of high affinity (pM) human renin inhibitors: application to analogues of ditekiren (U-71,038).
J Med Chem 34: 2107-12 (1991)
Upjohn Laboratories
Gastrin releasing peptide antagonists with improved potency and stability.
J Med Chem 34: 2102-7 (1991)
Merck Sharp & Dohme Research Laboratories
Identification and synthesis of a receptor binding site of human anaphylatoxin C5a.
J Med Chem 34: 2068-71 (1991)
Abbott Laboratories
Renin inhibitors containing esters at the P2-position. Oral activity in a derivative of methyl aminomalonate.
J Med Chem 34: 1935-43 (1991)
Warner-Lambert
Design of enzyme inhibitors using iterative protein crystallographic analysis.
J Med Chem 34: 1925-34 (1991)
Agouron Pharmaceuticals
Isoprenyl phosphinylformates: new inhibitors of squalene synthetase.
J Med Chem 34: 1912-4 (1991)
Bristol-Myers Squibb Pharmaceutical Research Institute
New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors: 5-substituted thieno[2,3-b]thiophene-2-sulfonamides and 5-substituted thieno[3,2-b]thiophene-2-sulfonamides.
J Med Chem 34: 1805-18 (1991)
Merck Sharp And Dohme Research Laboratories
Dexamethasone 21-(beta-isothiocyanatoethyl) thioether: a new affinity label for glucocorticoid receptors.
J Med Chem 34: 1762-7 (1991)
Niddk
Novel time-dependent inhibitors of human placental aromatase.
J Med Chem 34: 1748-50 (1991)
Marion Merrell Dow Research Institute
Synthesis and receptor binding of N-substituted tropane derivatives. High-affinity ligands for the cocaine receptor.
J Med Chem 34: 1728-31 (1991)
Research Biochemicals
Synthesis and hypocholesterolemic activity of 6,7-dihydro-4H-pyrazolo[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-diones, novel inhibitors of acylCoA:cholesterol O-acyltransferase.
J Med Chem 34: 1721-7 (1991)
Upjohn
Quinazoline antifolate thymidylate synthase inhibitors: heterocyclic benzoyl ring modifications.
J Med Chem 34: 1594-605 (1991)
Ici Pharmaceuticals Group
Structure-activity studies on a potent antagonist to organophosphate-induced toxicity.
J Med Chem 34: 1582-4 (1991)
University Of Iowa
Phosphonate-containing inhibitors of tyrosine-specific protein kinases.
J Med Chem 34: 1577-81 (1991)
National Cancer Institute-Bethesda
Novel site-directed affinity ligands for GABA-gated chloride channels: synthesis, characterization, and molecular modeling of 1-(isothiocyanatophenyl)-4-tert-butyl-2,6,7-trioxabicyclo[2.2.2]octanes .
J Med Chem 34: 1531-8 (1991)
National Institute Of Diabetes And Digestive And Kidney Diseases
Regulation of dopamine D2 receptors by sodium and pH.
Mol Pharmacol 39: 570-8 (1991)
Medical Research Service
1-(carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists.
J Med Chem 34: 1514-7 (1991)
Smithkline Beecham Pharmaceuticals
Quinazolinone cholecystokinin-B receptor ligands.
J Med Chem 34: 1505-8 (1991)
Eli Lilly
Novel caffeic acid derivatives: extremely potent inhibitors of 12-lipoxygenase.
J Med Chem 34: 1503-5 (1991)
Institute For Bio-Medical Research
New derivatives of kanamycin B obtained by combined modifications in positions 1 and 6". Synthesis, microbiological properties, and in vitro and computer-aided toxicological evaluation.
J Med Chem 34: 1483-92 (1991)
Katholieke Universiteit Leuven
New derivatives of kanamycin B obtained by modifications and substitutions in position 6''. 2. In vitro and computer-aided toxicological evaluation with respect to interactions with phosphatidylinositol.
J Med Chem 34: 1476-82 (1991)
Universit£
Synthesis and in vitro biological activity of new deaza analogues of folic acid, aminopterin, and methotrexate with an L-ornithine side chain.
J Med Chem 34: 1447-54 (1991)
Harvard Medical School
Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2.
J Med Chem 34: 1440-6 (1991)
Roche Research Center
Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen.
J Med Chem 34: 1436-40 (1991)
Research Triangle Institute
1,3,8-trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity.
J Med Chem 34: 1431-5 (1991)
Nova Pharmaceutical
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication.
J Med Chem 34: 1363-8 (1991)
Sri International
Inhibition of human placental aromatase by novel homologated 19-oxiranyl and 19-thiiranyl steroids.
J Med Chem 34: 1344-9 (1991)
Johns Hopkins University School Of Medicine
2-aralkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.
J Med Chem 34: 1340-4 (1991)
University Of South Florida
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.
J Med Chem 34: 1334-9 (1991)
University Of South Florida
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
J Med Chem 34: 1329-34 (1991)
Ciba-Geigy
N-[3H]methylscopolamine labeling of non-M1, non-M2 muscarinic receptor binding sites in rat brain.
J Pharmacol Exp Ther 256: 1173-81 (1991)
University Of California
Quinazoline antifolates inhibiting thymidylate synthase: 4-thio-substituted analogues.
J Med Chem 34: 978-84 (1991)
Institute Of Cancer Research
Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics.
J Med Chem 34: 887-900 (1991)
Merck Sharp And Dohme Research Laboratories
Synthesis and ligand binding of cocaine isomers at the cocaine receptor.
J Med Chem 34: 883-6 (1991)
Research Triangle Institute
Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors.
J Med Chem 34: 1228-30 (1991)
Merck Sharp And Dohme Research Laboratories
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
J Med Chem 34: 1225-8 (1991)
Merck Research Laboratories
Effect of hydroxyl group configuration in hydroxyethylamine dipeptide isosteres on HIV protease inhibition. Evidence for multiple binding modes.
J Med Chem 34: 1222-5 (1991)
University Of Wisconsin-Madison
Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor.
J Med Chem 34: 1209-21 (1991)
Roche Research Center
1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
J Med Chem 34: 1202-6 (1991)
Center For Bio-Pharmaceutical Sciences
Adenosine deaminase inhibitors: synthesis and structure-activity relationships of imidazole analogues of erythro-9-(2-hydroxy-3-nonyl)adenine.
J Med Chem 34: 1187-92 (1991)
Universit£
Carboxylic acids and tetrazoles as isosteric replacements for sulfate in cholecystokinin analogues.
J Med Chem 34: 1125-36 (1991)
Roche Research Center
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