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ID: ALA1136415

Journal: Bioorg Med Chem Lett

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

Authors: Zhou NE, Guo D, Thomas G, Reddy AV, Kaleta J, Purisima E, Menard R, Micetich RG, Singh R.

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.

CiteXplore: 12467634

DOI: 10.1016/s0960-894x(02)00831-4