title: Amino acid-derived phthalimide and saccharin derivatives as inhibitors of human leukocyte elastase, cathepsin G, and proteinase 3.
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.
authors.affiliation: Department of Chemistry, Wichita State University, Kansas 67260, USA.
authors.forename: W C
authors.initials: WC
authors.lastname: Groutas
authors.forename: L S
authors.initials: LS
authors.lastname: Chong
authors.forename: R
authors.initials: R
authors.lastname: Venkataraman
authors.forename: R
authors.initials: R
authors.lastname: Kuang
authors.forename: J B
authors.initials: JB
authors.lastname: Epp
authors.forename: N
authors.initials: N
authors.lastname: Houser-Archield
authors.forename: H
authors.initials: H
authors.lastname: Huang
authors.forename: J R
authors.initials: JR
authors.lastname: Hoidal
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001665:Binding Sites; D056649:Cathepsin G; D002403:Cathepsins / Q000037:antagonists & inhibitors*; D015195:Drug Design; D006801:Humans; D006860:Hydrogen Bonding; D066298:In Vitro Techniques; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics; D007962:Leukocytes / Q000201:enzymology; D008958:Models, Molecular; D008969:Molecular Sequence Data; D053146:Myeloblastin; D010797:Phthalimides / Q000737:chemistry / Q000494:pharmacology*; D011487:Protein Conformation; D012439:Saccharin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D012697:Serine Endopeptidases / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D010797:Phthalimides; D015842:Serine Proteinase Inhibitors; D002403:Cathepsins; D012697:Serine Endopeptidases; C534094:CTSG protein, human; D056649:Cathepsin G; D019272:Leukocyte Elastase; D053146:Myeloblastin; D012439:Saccharin