Title of article :
1-Alkoxycarbonyl-3-halogenoazetidin-2-ones as elastase (PPE) inhibitors Original Research Article
Author/Authors :
Stéphane Gérard، نويسنده , , Gaëtan Nollet، نويسنده , , Jennifer Vande Put، نويسنده , , Jacqueline Marchand-Brynaert، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2002
Abstract :
A series of 1-alkoxycarbonyl-3-halogenoazetidin-2-ones, designed as potential suicide inhibitors of serine proteases, has been synthesized and evaluated against porcine pancreatic elastase (PPE). All the compounds were transient inhibitors, their activity depending mainly on the nature of the halogen substituent: bromo- and iodo- derivatives are more active (Ki ∼2–22 μM) than 3-chloroazetidinones (Ki ∼20–150 μM). The lipophilicity of the N-1 substituent appeared to exert a slightly positive effect.
Journal title :
Bioorganic and Medicinal Chemistry
Journal title :
Bioorganic and Medicinal Chemistry