AMINO ACID-DERIVED PHTHALIMIDE AND SACCHARIN DERIVATIVES AS INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE, CATHEPSIN-G, AND PROTEINASE-3

Amino acid-derived phthalimide and saccharin derivatives have been inv estigated 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 e lastase and proteinase 3 (k(obs)/[I] values ranged between 180 and 362 0 M(-1) s(-1)) and showed weak or no inhibition toward cathepsin G. Th e corresponding phthalimide derivatives were found to be inactive. (C) 1996 Academic Press, Inc.