2014 Jan 28. pii: S0960-894X(14)00086-9. doi: 10.1016/j.bmcl.2014.01.056. [Epub ahead of print]
Switching cannabinoid response from CB2 agonists to FAAH inhibitors.
Tourteau A1, Leleu-Chavain N1, Body-Malapel M2, Andrzejak V1, Barczyk A1, Djouina M2, Rigo B3, Desreumaux P2, Chavatte P1, Millet R4.
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.
Copyright © 2014 Elsevier Ltd. All rights reserved.
Copyright © 2014 Elsevier Ltd. All rights reserved.
KEYWORDS:
CB(2), Cannabinoid, FAAH, IBD, Isoxazoles
- PMID:
- 24508127
- [PubMed – as supplied by publisher]
