GLUTAMINE-DERIVED ALDEHYDES FOR THE INHIBITION OF HUMAN RHINOVIRUS 3C PROTEASE

被引:43
作者
KALDOR, SW
HAMMOND, M
DRESSMAN, BA
LABUS, JM
CHADWELL, FW
KLINE, AD
HEINZ, BA
机构
[1] Lilly Research Laboratories, Eli Lilly and Company, Indianapolis
关键词
D O I
10.1016/0960-894X(95)00345-T
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Peptide aldehydes have been synthesized and evaluated as inhibitors of human rhinovirus 3C protease. Those inhibitors containing a C-terminal glutamine aldehyde were prepared using newly developed methodology involving reduction of the corresponding glutarimide, which can be easily prepared from N-protected glutamine. Low molecular weight (< 500) compounds with low to submicromolar inhibitory activity in both isolated enzyme and in vitro translation assays have been identified.
引用
收藏
页码:2021 / 2026
页数:6
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