Synthesis of (+)-biotin derivatives as HIV-1 protease inhibitors

被引：3
|
作者：
Han, Q
Lafontaine, J
Bacheler, LT
Rayner, MM
Klabe, RM
EricksonViitanen, S
Lam, PYS
机构：
[1] Chemical and Physical Sciences, The DuPont Merck Pharmaceutical Co., Experimental Station, Wilmington, DE 19880-0500
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 12期
关键词：
D O I：
10.1016/0960-894X(96)00233-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Several bis-N-alkylated (+)-biotin derivatives were synthesized and evaluated for activities against HIV-1 protease. The most potent inhibitor, 2D, synthesized in two steps from (+)-biotin, has K-i of 0.50 mu M and antiviral IC90 of 7 mu M. The (+)-biotin analogs in general have good translations from enzymatic K-i to antiviral cell assay IC90. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码：1371 / 1374
页数：4
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