Bioorganic & medicinal chemistry letters
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Bioorg. Med. Chem. Lett. · Jan 2003
3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.
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.