Tricyclic ureas: A new class of HIV-1 protease inhibitors

被引：116

作者：

Han, W ^{[1
]}

Pelletier, JC ^{[1
]}

Hodge, CN ^{[1
]}

机构：

[1] Dupont Merck Pharmaceut Co, Dept Chem & Phys Sci, Expt Stn, Wilmington, DE 19880 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(98)00659-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new class of tricyclic ureas containing a conformationally constrained proline was designed with the aid of molecular modeling. Efficient stereoselective intermolecular pinacol coupling represented the highlight of the synthesis. These rigid cyclic ureas are active towards HIV-1 protease, with 9 being the most potent compound (Ki = 9 nM) despite interacting with only three side chain binding pockets of HIV protease. (C) 1998 The DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.

引用

页码：3615 / 3620

页数：6

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