Studies on angiotensin converting enzyme inhibitors. VI. Synthesis and angiotensin converting enzyme inhibitory activities of the dicarboxylic acid derivative of imidapril and its diastereoisomers

DOI: 10.1248/cpb.40.1619

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1619 - 1622 (1992)

Update date:2022-07-29

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Authors:

Kubota Kubota

Nunami Nunami

Hayashi Hayashi

Hashimoto

Ogiku Ogiku

Matsuoka

Ishida Ishida

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Article abstract of DOI:10.1248/cpb.40.1619

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.

Full text of DOI:10.1248/cpb.40.1619

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