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

doi:10.1016/0960-894X(95)00037-T

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

Center for Drug Discovery

Research output: Contribution to journal › Article › peer-review

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 language	English
Pages (from-to)	367-370
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	5
Issue number	4
DOIs	https://doi.org/10.1016/0960-894X(95)00037-T
State	Published - Feb 16 1995

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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.",

author = "Denton Hoyer and Awad, {Mohamed M.A.} and Salvino, {Joseph M.} and Seoane, {Peter R.} and Dolle, {Roland E.} and Houck, {Wayne T.} and Sawutz, {David G.}",

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AU - Hoyer, Denton

AU - Awad, Mohamed M.A.

AU - Salvino, Joseph M.

AU - Seoane, Peter R.

AU - Dolle, Roland E.

AU - Houck, Wayne T.

AU - Sawutz, David G.

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Y1 - 1995/2/16

N2 - 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.

AB - 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.

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U2 - 10.1016/0960-894X(95)00037-T

DO - 10.1016/0960-894X(95)00037-T

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JF - Bioorganic and Medicinal Chemistry Letters

IS - 4

ER -

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

Abstract

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