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Bioorg Med Chem Lett. 2003 Jan 6;13(1):139-41.

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

Author information

1
SynPhar Laboratories, currently NAEJA Pharmaceutical Inc., 4290-91A Street, Edmonton, Alberta, Canada T6E 5V2.

Abstract

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-acylamino-azetidin-2-one derivatives showed very potent inhibition activities for cathepsins L, K and S at the nanomolar or subnanomolar IC(50) values.

PMID:
12467634
DOI:
10.1016/s0960-894x(02)00831-4
[Indexed for MEDLINE]

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