Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1′ substituents

被引：11
|
作者：
Kaltenbach, RF [1 ]
Klabe, RM [1 ]
Cordova, BC [1 ]
Seitz, SP [1 ]
机构：
[1] DuPont Pharmaceut Co, Expt Stn, Wilmington, DE 19880 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 15期
关键词：
antiproliferative agents; antivirals; enzyme inhibitors; substituent effects;
D O I：
10.1016/S0960-894X(99)00367-4
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of alkyl substituted P1/P1' analogs was prepared in an attempt to increase translation of the 3-aminoindazole class of HIV protease inhibitors. Increasing the lipophilicity of the P1/P1' residues dramatically improved translation of enzyme activity to antiviral activity in the whole cell assay. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2259 / 2262
页数：4
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