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  • Title: Efficient inhibition of human leukocyte elastase and cathepsin G by saccharin derivatives.
    Author: Groutas WC, Houser-Archield N, Chong LS, Venkataraman R, Epp JB, Huang H, McClenahan JJ.
    Journal: J Med Chem; 1993 Oct 15; 36(21):3178-81. PubMed ID: 8230105.
    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.
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