Search Results - "KOHN, T. J"
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Dibasic benzo[ b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 4. SAR studies on the conformationally restricted C3-side chain of hydroxybenzo[ b]thiophenes
Published in Bioorganic & medicinal chemistry letters (08-03-1999)“…A novel series of benzo[ b]thiophene diamine thrombin inhibitors with a conformationally restricted C3-side chain 3 was investigated. The constrained C3-side…”
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Diamino Benzo[b]thiophene Derivatives as a Novel Class of Active Site Directed Thrombin Inhibitors. 5. Potency, Efficacy, and Pharmacokinetic Properties of Modified C-3 Side Chain Derivatives
Published in Journal of medicinal chemistry (24-02-2000)“…A systematic investigation of the structure−activity relationships of the C-3 side chain of the screening hit 1a led to the identification of the potent…”
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Development of Dual-Acting Agents for Thromboxane Receptor Antagonism and Thromboxane Synthase Inhibition. 3. Synthesis and Biological Activities of Oxazolecarboxamide-Substituted ω-Phenyl-ω-(3-pyridyl)alkenoic Acid Derivatives and Related Compounds
Published in Journal of medicinal chemistry (31-12-1998)“…A novel series of oxazolecarboxamide-substituted ω-phenyl-ω-(3-pyridyl)alkenoic acid derivatives was discovered as potent dual-acting agents to block the TXA2…”
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Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. Part 6: Further focus on the contracted C4'-side chain analogues
Published in Bioorganic & medicinal chemistry letters (05-06-2000)“…Novel benzo[b]thiophene diamine thrombin inhibitors were investigated, focusing on a contracted C4'-side chain series. SAR studies identified compounds with…”
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Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 2. Design, synthesis, and evaluation of a novel series of phenyl oxazole derivatives
Published in Bioorganic & medicinal chemistry letters (04-08-1998)“…Synthesis and initial in vitro evaluation of a novel series of phenyl oxazole derivatives are described. An SAR study of the novel dual-acting TRA/TSI agent…”
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Dibasic benzo[ b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 2: sidechain optimization and demonstration of in vivo efficacy
Published in Bioorganic & medicinal chemistry letters (08-03-1999)“…Potent, subnanomolar thrombin inhibitors 4, 5, and 6 are developed through side chain optimization of novel, benzo[ b]thiophene-based small organic entities 2…”
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Advances toward new antidepressants beyond SSRIS: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 4
Published in Bioorganic & medicinal chemistry letters (17-05-2004)“…A series of 1-(1H-indol-4-yloxy)-3-(4-arylpiperidinyl)propan-2-ols possessing potent dual 5-HT(1A) receptor antagonism and serotonin reuptake inhibition was…”
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Advances toward new antidepressants beyond SSRIs : 1-Aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 5
Published in Bioorganic & medicinal chemistry letters (01-05-2006)“…A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT1A receptor antagonism and serotonin reuptake inhibition was discovered…”
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Advances toward new antidepressants beyond SSRIs: 1-Aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 1
Published in Bioorganic & medicinal chemistry letters (02-06-2003)“…A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT(1A) receptor antagonism and serotonin reuptake inhibition was discovered…”
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Advances toward new antidepressants beyond SSRIS: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 3
Published in Bioorganic & medicinal chemistry letters (17-11-2003)“…A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT(1A) receptor antagonism and serotonin reuptake inhibition was discovered…”
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