3-酰基氨基氮杂环丁烷-2-酮作为一类新型半胱氨酸蛋白酶抑制剂。
3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.
作者信息
Zhou Nian E, Guo Deqi, Thomas George, Reddy Andhe V N, Kaleta Jadwiga, Purisima Enrico, Menard Robert, Micetich Ronald G, Singh Rajeshwar
机构信息
SynPhar Laboratories, currently NAEJA Pharmaceutical Inc., 4290-91A Street, Edmonton, Alberta, Canada T6E 5V2.
出版信息
Bioorg Med Chem Lett. 2003 Jan 6;13(1):139-41. doi: 10.1016/s0960-894x(02)00831-4.
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.
描述了一类新型的半胱氨酸蛋白酶组织蛋白酶B、L、K和S的抑制剂。这些抑制剂基于β-内酰胺环设计，旨在与半胱氨酸蛋白酶活性位点中半胱氨酸的亲核硫醇相互作用。一些3-酰基氨基氮杂环丁烷-2-酮衍生物对组织蛋白酶L、K和S表现出非常强的抑制活性，其半数抑制浓度（IC50）值在纳摩尔或亚纳摩尔范围内。
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