| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369902 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
A series of 3-carboxamido-5-aryl-isoxazoles designed as CB2 agonists were evaluated as FAAH inhibitors. The pharmacological results led to identify structure–activity relationships enabling to switch cannabinoid response from CB2 agonists to FAAH inhibitors. Two compounds were selected for their FAAH and/or CB2 activity, and evaluated in a colitis model for their anti-inflammatory activity. Results showed that compounds 10 and 11 inhibit the development of DSS-induced acute colitis in mice and then, are interesting leads to explore new drug candidates for IBD.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Aurélien Tourteau, Natascha Leleu-Chavain, Mathilde Body-Malapel, Virginie Andrzejak, Amélie Barczyk, Madjid Djouina, Benoit Rigo, Pierre Desreumaux, Philippe Chavatte, Régis Millet,