Ace inhibitors as a template for the design of bradykinin B2 receptor antagonists

Denton Hoyer, Mohamed M.A. Awad, Joseph M. Salvino, Peter R. Seoane, Roland E. Dolle, Wayne T. Houck, David G. Sawutz

Research output: Contribution to journalArticle

14 Scopus citations

Abstract

Angiotensin converting enzyme (ACE) degrades both angiotensin II and bradykinin. Accordingly, we hypothesize that ACE inhibitors can serve as models to design antagonists for the bradykinin receptor. The potent ACE inhibitor Quinapril was modified to serve as a spacer separating two lipophilic positive charges required for bradykinin binding. The synthesis and bradykinin receptor activity of a series of antagonists 2-10 based on this hypothesis is described in this report.

Original languageEnglish
Pages (from-to)367-370
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume5
Issue number4
DOIs
StatePublished - Feb 16 1995
Externally publishedYes

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