Synthesis and in vitro evaluation of pseudosaccharinamine derivatives as potential elastase inhibitors.
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.
Rode
Haridas
H
Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Ernst-Moritz-Arndt-University, Friedrich-Ludwig-Jahn-Str. 17, D-17489 Greifswald, Germany.
Koerbe
Stefanie
S
Besch
Anita
A
Methling
Karen
K
Loose
Jutta
J
Otto
Hans-Hartwig
HH
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
D004791:Enzyme Inhibitors; C511580:pseudosaccharinamine; D019272:Leukocyte Elastase; D012439:Saccharin