The synthesis and evaluation of cyclic ureas as HIV protease inhibitors:: Modifications of the P1/P1′ residues

被引：29
|
作者：
Patel, M
Bacheler, LT
Rayner, MM
Cordova, BC
Klabe, RM
Erickson-Viitanen, S
Seitz, SP
机构：
[1] Dupont Merck Pharmaceut Co, Expt Stn, Dept Chem & Phys Sci, Wilmington, DE 19880 USA
[2] Dupont Merck Pharmaceut Co, Expt Stn, Dept Virol, Wilmington, DE 19880 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 07期
关键词：
D O I：
10.1016/S0960-894X(98)00119-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Two series of cyclic ureas modified at the P1/P1' residue were prepared and evaluated for HIV protease inhibition and whole cell antiviral activity. Compounds 8b, 10 (3- and 4-pyridylmethyl analogs) and 6b (4-methoxy analog) showed significant improvement in antiviral activity relative to lead compounds DMP323 and DMP 450. (C) 1998 The DuPont Merck Pharmaceutical Company. Published by Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：823 / 828
页数：6
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