Nonpeptide angiotensin II receptor antagonists: the discovery of a series of N-(biphenylylmethyl) imidazoles as potent, orally active antihypertensives

DJ Carini, JV Duncia, PE Aldrich, AT Chiu…

Index: Carini, David J.; Duncia, John V.; Aldrich, Paul E.; Chiu, Andrew T.; Johnson, Alexander L.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2525 - 2547

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Citation Number: 454

Abstract

Discussion Compounds with the core structure 1 have previously been found to be potent antagonists of the AI1 receptor and to be antihypertensive upon iv administrations3 Replacement of the polar carboxylic acid group (A) with acid isosteres of greater lipophilicity, such as NHS02CF3, resulted in some oral activity. However, none of these compounds when dosed orally produced an effect to compare with their intravenous antihypertensive ...