Design and synthesis of dipeptidyl α′,β′-epoxy ketones, potent irreversible inhibitors of the cysteine protease cruzain

被引：45

作者：

Roush, WR ^{[1
]}

González, FV

McKerrow, JH

Hansell, E

机构：

[1] Univ Michigan, Dept Chem, Ann Arbor, MI 48109 USA

[2] Univ Calif San Francisco, Dept Pathol, San Francisco, CA 94121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(98)00494-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The dipeptidyl epoxy ketone 4 is a potent, irreversible inhibitor of cruzain, a cysteine protease isolated from Trypanosoma cruzi, with an apparent second order inhibition rate constant of 330,000 sec(-1)M(-1). (C) 1998 Elsevier Science Ltd. All rights reserved.

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页码：2809 / 2812

页数：4

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