Title of article :
Amino Acid-Derived Phthalimide and Saccharin Derivatives as Inhibitors of Human Leukocyte Elastase, Cathepsin G, and Proteinase 3
Author/Authors :
Groutas، نويسنده , , William C. F. Chong، نويسنده , , Lee S. and Venkataraman، نويسنده , , Radhika and Kuang، نويسنده , , Rongze and Epp، نويسنده , , Jeff B. and Houser-Archield، نويسنده , , Nadene and Huang، نويسنده , , He and Hoidal، نويسنده , , John R.، نويسنده ,
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 3620M−1s−1) and showed weak or no inhibition toward cathepsin G. The corresponding phthalimide derivatives were found to be inactive.
