Potent cyclic urea HIV protease inhibitors with benzofused heterocycles as P2/P2' groups

被引：104

作者：

Rodgers, JD

Johnson, BL

Wang, HS

Greenberg, RA

EricksonViitanen, S

Klabe, RM

Cordova, BC

Rayner, MM

Lam, GN

Chang, CH

机构：

[1] DuPont Merck Pharmaceutical Company, E500/4603 Experimental Station, Wilmington, DE 19880-0500

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(96)00531-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of benzofused heterocycles was examined to replace the metabolically unstable benzyl alcohol P2/P2' groups of DMP 323 (1). Extremely potent inhibitors of HIV protease (Ki < 0.01 nM) and excellent antiviral activity (IC90 = 8 nM) were found. An X-ray crystal structure of benzimidazolone 5a bound to HIV protease showed H-bonds to Asp30 and a bridging water molecule to Gly48. Copyright (C) 1996 The DuPont Merck Pharmaceutical Company. Published by Elsevier Science Ltd

引用

页码：2919 / 2924

页数：6

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