Potent nonpeptide angiotensin II receptor antagonists. 2. 1-(Carboxybenzyl) imidazole-5-acrylic acids

RM Keenan, J Weinstock, JA Finkelstein…

Index: Keenan, Richard M.; Weinstock, Joseph; Finkelstein, Joseph A.; Franz, Robert G.; Gaitanopoulos, Dimitri E.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 13 p. 1880 - 1892

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Citation Number: 73

Abstract

The further evolution of the imidazole-5-acrylic acid series of nonpeptide angiotensin I1 receptor antagonists is detailed (for Part 1, see: J. Med. Chem. 1992, 35, 3858). Modifications of the N-benzyl ring substitution were undertaken in an effort to mimic the Tyr4 residue of angiotensin 11. Introduction of ap-carboxylic acid on the N-benzyl ring resulted in the discovery of compounds with nanomolar affinity for the receptor and good oral activity. ...