Studies on Angiotensin Converting Enzyme Inhibitors. VI. Synthesis and Angiotensin Converting Enzyme Inhibitory Activities of the Dicarboxylic Acid Derivative of Imidapril and Its Diastereoisomers

Hitoshi KUBOTA; Ken-ichi NUNAMI; Kimiaki HAYASHI; Yoshikatsu HASHIMOTO; Noriko OGIKU; Yuzo MATSUOKA; Ryuichi ISHIDA

doi:10.1248/cpb.40.1619

Hitoshi KUBOTA, Ken-ichi NUNAMI, Kimiaki HAYASHI, Yoshikatsu HASHIMOTO, Noriko OGIKU, Yuzo MATSUOKA, Ryuichi ISHIDA

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Keywords: ACE inhibitor, imidapril, enalapril, biologically active form

JOURNAL FREE ACCESS

1992 Volume 40 Issue 6 Pages 1619-1622

DOI https://doi.org/10.1248/cpb.40.1619

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Abstract

All possible diastereoisomers of the dicarboxylic acid (10a), the biologically active form of imidapril (1), were synthesized, and their inhibitory activity against angiotensin converting enzyme (ACE) was examined. The in vitro ACE inhibitory activity of these compounds greatly depended on the configurations of the three asymmetric carbons in each molecule. The (S, S, S) isomer (10a) showed much more potent activity than the others.

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