NOVEL PSEUDOSYMMETRIC INHIBITORS OF HIV-1 PROTEASE

被引：12
|
作者：
FASSLER, A
ROSEL, J
GRUTTER, M
TINTELNOTBLOMLEY, M
ALTERI, E
BOLD, G
LANG, M
机构：
[1] Research Laboratories, Pharmaceutical Division, Ciba-Geigy Ltd.
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 12期
关键词：
D O I：
10.1016/S0960-894X(01)80775-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Compounds containing the easily accessible Phe[CH(OH)CH2N(NH)]Phe dipeptide isostere as a non-hydrolyzable replacement of the scissile amide bond in the natural substrate are potent inhibitors of HIV-1 protease. The expected symmetric binding pattern of the most potent inhibitor in this series (CGP 53820, IC50 = 9 nM) is illustrated by the X-ray analysis performed with the corresponding enzyme-inhibitor complex.
引用
收藏
页码：2837 / 2842
页数：6
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