3-acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors

被引：62
作者：
Zhou, NE
Guo, DQ
Thomas, G
Reddy, AVN
Kaleta, J
Purisima, E
Menard, R
Micetich, RG
Singh, R
机构：
[1] Natl Res Council Canada, Biotechnol Res Inst, Montreal, PQ H4P 2R2, Canada
[2] NAEJA Pharmaceut Inc, SynPhar Labs, Edmonton, AB T6E 5V2, Canada
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 01期
关键词：
D O I：
10.1016/S0960-894X(02)00831-4
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new class of inhibitors for cysteine proteases cathepsin B, L, K and S is described. These inhibitors are based on the beta-lactam ring designed to interact with the nucleophilic thiol of the cysteine in the active site of cysteine proteases. Some 3-acylaminoazetidin-2-one derivatives showed very potent inhibition activities for cathepsins L, K and S at the nanomolar or subnanomolar IC50 values. (C) 2002 Elsevier Science Ltd. All rights reserved.
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页码：139 / 141
页数：3
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