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
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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