title: New FAAH inhibitors based on 3-carboxamido-5-aryl-isoxazole scaffold that protect against experimental colitis.
abstract: 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 (IC(50)=0.088 μM) and reduced colitis induced by intrarectal administration of TNBS.
authors: Université Lille Nord de France, ICPAL, EA 4481, IFR114, 3 rue du Professeur Laguesse, BP-83, F-59006 Lille, France.
authors: Virginie
authors: V
authors: Andrzejak
authors: Giulio G
authors: GG
authors: Muccioli
authors: Mathilde
authors: M
authors: Body-Malapel
authors: Jamal
authors: J
authors: El Bakali
authors: Madjid
authors: M
authors: Djouina
authors: Nicolas
authors: N
authors: Renault
authors: Philippe
authors: P
authors: Chavatte
authors: Pierre
authors: P
authors: Desreumaux
authors: Didier M
authors: DM
authors: Lambert
authors: Régis
authors: R
authors: Millet