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

页码：2837 / 2842

页数：6

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