1. 3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.
- Author
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Zhou NE, Guo D, Thomas G, Reddy AV, Kaleta J, Purisima E, Menard R, Micetich RG, and Singh R
- Subjects
- Azetidines pharmacology, Cathepsin B antagonists & inhibitors, Cathepsin K, Cathepsin L, Cathepsins antagonists & inhibitors, Cysteine Endopeptidases, Cysteine Proteinase Inhibitors pharmacology, Drug Design, Humans, Inhibitory Concentration 50, Lactams chemistry, Leukocyte Elastase antagonists & inhibitors, Structure-Activity Relationship, Azetidines chemical synthesis, Cysteine Proteinase Inhibitors chemical synthesis
- 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.
- Published
- 2003
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