Small peptidic aldehyde inhibitors of human rhinovirus 3C protease

被引:42
作者
Shepherd, TA
Cox, GA
McKinney, E
Tang, J
Wakulchik, M
Zimmerman, RE
Villarreal, EC
机构
[1] Lilly Research Laboratories, Eli Lilly and Company, Indianapolis
关键词
D O I
10.1016/S0960-894X(96)00537-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Small peptide aldehydes were designed to mimic the preferred substrate requirements for the human rhinovirus 3C protease. Di- and tripeptide aldehydes containing a methionine sulfone as a P-1 surrogate for glutamine show low micromolar enzyme inhibitory and antiviral tissue culture activity. LY338387, obtained in a short and efficient synthesis, appears to validate the protease as a therapeutic target. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:2893 / 2896
页数:4
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