| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365031 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
A series of novel 2-azetidinones (β-lactams) bearing short alkenyl chains at C3 and N1 have been prepared and evaluated in vitro as inhibitors of human FAAH. Compound 9c (1-(4′-pentenoyl-3-(4′-pentenyl)-2-azetidinone)) featured an IC50 value of 4.5 μM and a good selectivity for FAAH versus MGL.
Graphical abstractThe evaluation of lipophilic 2-azetidinone derivatives as FAAH/MGL potential inhibitors is reported for the first time. One compound (9c) is a good and selective inhibitor of FAAH.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Allan Urbach, Giulio G. Muccioli, Eric Stern, Didier M. Lambert, Jacqueline Marchand-Brynaert,