title: Studies on angiotensin converting enzyme inhibitors. VI. Synthesis and angiotensin converting enzyme inhibitory activities of the dicarboxylic acid derivative of imidapril and its diastereoisomers.
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.
authors.affiliation: Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd., Osaka, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Kubota
authors.forename: K
authors.initials: K
authors.lastname: Nunami
authors.forename: K
authors.initials: K
authors.lastname: Hayashi
authors.forename: Y
authors.initials: Y
authors.lastname: Hashimoto
authors.forename: N
authors.initials: N
authors.lastname: Ogiku
authors.forename: Y
authors.initials: Y
authors.lastname: Matsuoka
authors.forename: R
authors.initials: R
authors.lastname: Ishida
mesh_terms: D000806:Angiotensin-Converting Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D048289:Imidazolidines; D066298:In Vitro Techniques; D007672:Kidney Cortex / Q000187:drug effects; D013237:Stereoisomerism; D013552:Swine
chemical_list: D000806:Angiotensin-Converting Enzyme Inhibitors; D007093:Imidazoles; D048289:Imidazolidines; C065166:imidapril