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Switching cannabinoid response from CB2 agonists to FAAH inhibitors

Archive ouverte : Article de revue

Tourteau, Aurélien | Leleu-Chavain, Natascha | Body-Malapel, Mathilde | Andrzejak, Virginie | Barczyk, Amelie | Djouina, Madjid | Rigo, Benoit | Desreumaux, Pierre | Chavatte, Philippe | Millet, Régis

Edité par HAL CCSD ; Elsevier

International audience. 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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