Author/Authors :
Nian E. Zhou، نويسنده , , Deqi Guo، نويسنده , , K. George Thomas، نويسنده , , Andhe V. N. Reddy، نويسنده , , Jadwiga Kaleta، نويسنده , , Enrico Purisima، نويسنده , , Robert Menard، نويسنده , , Ronald G. Micetich، نويسنده , , Rajeshwar Singh، نويسنده ,
Abstract :
A new class of inhibitors for cysteine proteases cathepsin B, L, K and S is described. These inhibitors are based on the β-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 IC50 values.