Cyclic urea HIV protease inhibitors containing alkynyl- and alkenyl-tethered heterocycles in the P2 region

被引：17

作者：

Dax, SL

Cook, SC

机构：

[1] Dept. of Chem. and Physical Sciences, Dupont Merck Pharmaceutical Company, Wilmington

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 07期

关键词：

D O I：

10.1016/0960-894X(96)00108-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of cyclic urea HIV protease inhibitors containing alkynyl- and allrenyl-tethered heterocycles in the P2 region were synthesized The alkynyl compounds exhibited poor activity against the HN protease enzyme. However, reduction of the triple bond afforded trans-alkenyl derivatives (XU348 and XU430) which displayed superb potency (sub-nanomolar K-i). Copyright (C) 1996 Elsevier Science Ltd

引用

页码：797 / 802

页数：6

共 4 条

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[4] 1995, SCRIP 1227, P21

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