title: 3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.
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.
authors.affiliation: SynPhar Laboratories, currently NAEJA Pharmaceutical Inc., 4290-91A Street, Edmonton, Alberta, Canada T6E 5V2.
authors.forename: Nian E
authors.initials: NE
authors.lastname: Zhou
authors.forename: Deqi
authors.initials: D
authors.lastname: Guo
authors.forename: George
authors.initials: G
authors.lastname: Thomas
authors.forename: Andhe V N
authors.initials: AV
authors.lastname: Reddy
authors.forename: Jadwiga
authors.initials: J
authors.lastname: Kaleta
authors.forename: Enrico
authors.initials: E
authors.lastname: Purisima
authors.forename: Robert
authors.initials: R
authors.lastname: Menard
authors.forename: Ronald G
authors.initials: RG
authors.lastname: Micetich
authors.forename: Rajeshwar
authors.initials: R
authors.lastname: Singh
mesh_terms: D001384:Azetidines / Q000138:chemical synthesis* / Q000494:pharmacology; D002401:Cathepsin B / Q000037:antagonists & inhibitors; D056657:Cathepsin K; D056668:Cathepsin L; D002403:Cathepsins / Q000037:antagonists & inhibitors; D003546:Cysteine Endopeptidases; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D007769:Lactams / Q000737:chemistry; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
chemical_list: D001384:Azetidines; D015853:Cysteine Proteinase Inhibitors; D007769:Lactams; D002403:Cathepsins; D019272:Leukocyte Elastase; D003546:Cysteine Endopeptidases; D002401:Cathepsin B; C534281:CTSL protein, human; D056668:Cathepsin L; C028217:cathepsin S; C534130:CTSK protein, human; D056657:Cathepsin K