Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 12, Pages 3777-3786Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.04.057
Keywords
FAAH; Cannabinoids; IBD; Isoxazole; FAAH modeling
Funding
- Conseil Regional Nord Pas de Calais
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Growing evidence suggests a role for the endocannabinoid (EC) system, in intestinal inflammation and compounds inhibiting anandamide degradation offer a promising therapeutic option for the treatment of inflammatory bowel diseases. In this paper, we report the first series of carboxamides derivatives possessing FAAH inhibitory activities. Among them, compound 39 displayed significant inhibitory FAAH activity (IC50 = 0.088 mu M) and reduced colitis induced by intrarectal administration of TNBS. (C) 2011 Elsevier Ltd. All rights reserved.
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