New carboxyalkyl inhibitors of brain enkephalinase: Synthesis, biological activity and analgesic properties

…, E Soroca-Lucas, H Marcais-Collado…

Index: Fournie Zaluski; Chaillet; Soroca Lucas; Fournie-Zaluski; Marcais-Collado; Costentin; Roques Journal of Medicinal Chemistry, 1983 , vol. 26, # 1 p. 60 - 65

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Citation Number: 29

Abstract

New carboxyalkyl compounds derived from Phe-Leu and Phe-Ala were synthesized and checked as inhibitors of “enkephalinase”, a metalloendopeptidase cleaving the Gly-Phe4 bond of enkephalins from mouse striatal membranes. Differential recognition of both brain enkephalinase and angiotensin-converting enzyme (ACE) catalytic sites by these carboxylalkyl compounds lead to potent (KI= 0.5 pM), competitive and selective inhibitors ...