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Updated: Aug 9, 2026

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Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase
Published on: November 23, 2016
Synthesis and in vitro evaluation of pseudosaccharinamine derivatives as potential elastase inhibitors
Haridas Rode1, Stefanie Koerbe, Anita Besch
1Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Ernst-Moritz-Arndt-University, Friedrich-Ludwig-Jahn-Str. 17, D-17489 Greifswald, Germany.
Bioorganic & Medicinal Chemistry
|December 27, 2005
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.

