title: Efficient inhibition of human leukocyte elastase and cathepsin G by saccharin derivatives.
abstract: A series of saccharin derivatives I has been synthesized and evaluated for their inhibitory activity toward human leukocyte elastase and cathepsin G. Most of the compounds were found to be efficient and time-dependent inhibitors of elastase. Inactivated elastase was found to regain its activity almost fully after 24 h (80-90% activity) and the half-lives of reactivation ranged between 12-15 h. Addition of hydroxylamine to fully-inactivated enzyme led to rapid and complete recovery of enzymatic activity. A tentative mechanism of action is proposed on the basis of biochemical and model studies.
authors.affiliation: Department of Chemistry, Wichita State University, Kansas 67260.
authors.forename: W C
authors.initials: WC
authors.lastname: Groutas
authors.forename: N
authors.initials: N
authors.lastname: Houser-Archield
authors.forename: L S
authors.initials: LS
authors.lastname: Chong
authors.forename: R
authors.initials: R
authors.lastname: Venkataraman
authors.forename: J B
authors.initials: JB
authors.lastname: Epp
authors.forename: H
authors.initials: H
authors.lastname: Huang
authors.forename: J J
authors.initials: JJ
authors.lastname: McClenahan
mesh_terms: D056649:Cathepsin G; D002403:Cathepsins / Q000037:antagonists & inhibitors*; D006801:Humans; D019272:Leukocyte Elastase; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D012439:Saccharin / Q000031:analogs & derivatives*; D012697:Serine Endopeptidases; D013329:Structure-Activity Relationship
chemical_list: D002403:Cathepsins; D012697:Serine Endopeptidases; C534094:CTSG protein, human; D056649:Cathepsin G; D010196:Pancreatic Elastase; D019272:Leukocyte Elastase; D012439:Saccharin