Amino acid-derived phthalimide and saccharin derivatives as inhibitors of human leukocyte elastase, cathepsin G, and proteinase 3

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Issue Date
1996-08-15
Authors
Groutas, William C.
Chong, Lee S.
Venkataraman, Radhika
Kuang, Rongze
Epp, Jeffrey B.
Houser-Archield, Nadene
Huang, He
Hoidal, John R.
Advisor
Citation

Archives of biochemistry and biophysics. 1996 Aug 15; 332(2): 335-40.

Abstract

Amino acid-derived phthalimide and saccharin derivatives have been investigated for their inhibitory activity toward the serine proteinases human leukocyte elastase, cathepsin G, and proteinase 3. The saccharin derivatives were found to be effective time-dependent inhibitors of elastase and proteinase 3 (kobs/[I] values ranged between 180 and 3620 M-1 S-1) and showed weak or no inhibition toward cathepsin G. The corresponding phthalimide derivatives were found to be inactive.

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