title: Synthesis and in vitro evaluation of pseudosaccharinamine derivatives as potential elastase inhibitors.
abstract: Pseudosaccharinamine derivatives were evaluated for elastase inhibitory activity. Ester derivatives of pseudosaccharinamine displayed reversible and high inhibition of human leukocyte elastase (HLE) as compared to porcine pancreatic elastase (PPE). Cyanomethyl (2S,3S)-2-(1,1-dioxobenzo[d]isothiazol-3-ylamino)-3-methylpentanoate was found to inhibit HLE at Ki=0.8 microM.
authors.affiliation: Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Ernst-Moritz-Arndt-University, Friedrich-Ludwig-Jahn-Str. 17, D-17489 Greifswald, Germany.
authors.forename: Haridas
authors.initials: H
authors.lastname: Rode
authors.forename: Stefanie
authors.initials: S
authors.lastname: Koerbe
authors.forename: Anita
authors.initials: A
authors.lastname: Besch
authors.forename: Karen
authors.initials: K
authors.lastname: Methling
authors.forename: Jutta
authors.initials: J
authors.lastname: Loose
authors.forename: Hans-Hartwig
authors.initials: HH
authors.lastname: Otto
mesh_terms: D002851:Chromatography, High Pressure Liquid; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy; D012439:Saccharin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; C511580:pseudosaccharinamine; D019272:Leukocyte Elastase; D012439:Saccharin