RENIN INHIBITORS CONTAINING ISOSTERIC REPLACEMENTS OF THE AMIDE BOND CONNECTING THE P3 AND P2 SITES

被引：85

作者：

KALTENBRONN, JS ^{[1
]}

HUDSPETH, JP ^{[1
]}

LUNNEY, EA ^{[1
]}

MICHNIEWICZ, BM ^{[1
]}

NICOLAIDES, ED ^{[1
]}

REPINE, JT ^{[1
]}

ROARK, WH ^{[1
]}

STIER, MA ^{[1
]}

TINNEY, FJ ^{[1
]}

WOO, PKW ^{[1
]}

ESSENBURG, AD ^{[1
]}

机构：

[1] WARNER LAMBERT PARKE DAVIS, PARKE DAVIS PHARMACEUT RES DIV, DEPT PHARMACOL, ANN ARBOR, MI 48105 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 33卷 / 02期

关键词：

D O I：

10.1021/jm00164a058

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Renin inhibitors having 13 different isosteres connecting the P3 and P2 positions have been prepared. Synthetic routes and in vitro activity exhibited by these compounds are discussed. The two most potent compounds, 47 and 48, contained the hydroxyethylene isostere, Ψ[CHOHCH2], and had IC50 values of 61 and 22 nM, respectively. © 1990, American Chemical Society. All rights reserved.

引用

页码：838 / 845

页数：8

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