Efficient inhibition of human leukocyte elastase and cathepsin G by saccharin derivatives

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Groutas, William C.
Houser-Archield, Nadene
Chong, Lee S.
Venkataraman, Radhika
Epp, Jeffrey B.
Huang, He
McClenahan, Jerald J.

Journal of medicinal chemistry. 1993 Oct 15; 36(21): 3178-81.


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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