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

Autor:	Robert Menard, Rajeshwar Singh, Nian E. Zhou, Jadwiga Kaleta, Ronald G. Micetich, Enrico O. Purisima, George Thomas, Deqi Guo, Andhe V. Narender Reddy
Rok vydání:	2002
Předmět:	Proteases Lactams Stereochemistry Cathepsin L Clinical Biochemistry Cathepsin K Pharmaceutical Science Cysteine Proteinase Inhibitors Biochemistry Cathepsin B Deubiquitinating enzyme Inhibitory Concentration 50 Structure-Activity Relationship Nucleophile Drug Discovery pharmaceutical Humans Molecular Biology genome Cathepsin S Cathepsin chemistry.chemical_classification biology Organic Chemistry Active site General Medicine Cathepsins Cysteine Endopeptidases chemistry Enzyme inhibitor Drug Design biology.protein Thiol Molecular Medicine Azetidines Leukocyte Elastase Cysteine
Zdroj:	Bioorganicmedicinal chemistry letters. 13(1)
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cbf662c970730d120e0983f782b63970 https://pubmed.ncbi.nlm.nih.gov/12467634 Zobrazit plný text záznamu Full Text from ScienceDirect