Synthesis and biological activity of novel potent endothelin-converting enzyme-1 inhibitors

被引：12

作者：

Firooznia, F ^{[1
]}

Gude, C ^{[1
]}

Chan, K ^{[1
]}

Fink, CA ^{[1
]}

Qiao, Y ^{[1
]}

Satoh, Y ^{[1
]}

Marcopoulos, N ^{[1
]}

Savage, P ^{[1
]}

Beil, ME ^{[1
]}

Bruseo, CW ^{[1
]}

Trapani, AJ ^{[1
]}

Jeng, AY ^{[1
]}

机构：

[1] Novartis Inst Biomed Res, Summit, NJ 07901 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(00)00657-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Through directed screening of metalloprotease inhibitors. CGS 30084 (1) has been identified as a potent endothelin-converting enzyme-1 (ECE-1) inhibitor in vitro (IC50 = 77 nM). Herein we report the synthesis and biological activities of analogues derived from this lead. based on modifications of the biphenyl moiety. Compound 10. the thioacetate methyl ester prodrug derivative of compound 6m. was found to he an orally active and potent inhibitor of ECE-1 activity in rats. (C) 2001 Elsevier science Ltd. All rights reserved.

引用

页码：375 / 378

页数：4

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