Discovery and Evaluation of a Series of 3-Acylindole Imidazopyridine Platelet-Activating Factor Antagonists 1

…, GM Carrera, DH Steinman, JA Trautmann…

Index: Curtin, Michael L.; Davidsen, Steven K.; Heyman, H. Robin; Garland, Robert B.; Sheppard, George S.; Florjancic, Alan S.; Xu, Lianhong; Carrera Jr., George M.; Steinman, Douglas H.; Trautmann, Jeff A.; Albert, Daniel H.; Magoc, Terrance J.; Tapang, Paul; Rhein, David A.; Conway, Richard G.; Luo, Gongjin; Denissen, Jon F.; Marsh, Kennan C.; Morgan, Douglas W.; Summers, James B. Journal of Medicinal Chemistry, 1998 , vol. 41, # 1 p. 74 - 95

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Citation Number: 31

Abstract

Studies conducted with the goal of discovering a second-generation platelet-activating factor (PAF) antagonist have identified a novel class of potent and orally active antagonists which have high aqueous solubility and long duration of action in animal models. The compounds arose from the combination of the lipophilic indole portion of Abbott's first-generation PAF antagonist ABT-299 (2) with the methylimidazopyridine heterocycle moiety of British ...

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4-(2-Methyl-1H-imidazo[4,5-c]pyridin-1-yl)benzonitrile Structure

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4-ethynyl-3-[3-fluoro-4-[(2-methylimidazo[4,5-c]pyridin-1-yl)methyl]benzoyl]-N,N-dimethylindole-1-carboxamide Structure

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4-ethynyl-3-[3-fluoro-4-[(2-methylimidazo[4,5-c]pyridin-1-yl)methyl]benzoyl]-N,N-dimethylindole-1-carboxamide Structure

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4-ethynyl-3-[3-fluoro-4-[(2-methylimidazo[4,5-c]pyridin-1-yl)methyl]benzoyl]-N,N-dimethylindole-1-carboxamide Structure

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4-ethynyl-3-[3-fluoro-4-[(2-methylimidazo[4,5-c]pyridin-1-yl)methyl]benzoyl]-N,N-dimethylindole-1-carboxamide Structure

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~%

4-ethynyl-3-[3-fluoro-4-[(2-methylimidazo[4,5-c]pyridin-1-yl)methyl]benzoyl]-N,N-dimethylindole-1-carboxamide Structure

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3-[4-(aminomethyl)-3-fluorobenzoyl]-4-bromo-N,N-dimethylindole-1-carboxamide Structure

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4-bromo-3-[3-fluoro-4-[[(3-nitropyridin-4-yl)amino]methyl]benzoyl]-N,N-dimethylindole-1-carboxamide Structure

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54079-68-4

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