ACE-INHIBITORS AS A TEMPLATE FOR THE DESIGN OF BRADYKININ B-2 RECEPTOR ANTAGONISTS

被引：13

作者：

HOYER, D

AWAD, MMA

SALVINO, JM

SEOANE, PR

DOLLE, RE

HOUCK, WT

SAWUTZ, DG

机构：

[1] STERLING WINTHROP PHARMACEUT RES DIV,DEPT MED CHEM,COLLEGEVILLE,PA 19426

[2] STERLING WINTHROP PHARMACEUT RES DIV,DEPT BIOCHEM,COLLEGEVILLE,PA 19426

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 04期

关键词：

D O I：

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

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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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页码：367 / 370

页数：4

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