Efficient Inhibition of Human Leukocyte Elastase and Cathepsin G by Saccharin Derivatives

Article abstract of DOI:10.1021/jm00073a019

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 percent 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.