Canna~Fangled Abstracts

Switching cannabinoid response from CB2 agonists to FAAH inhibitors.

By January 28, 2014 No Comments
2014 Jan 28. pii: S0960-894X(14)00086-9. doi: 10.1016/j.bmcl.2014.01.056. [Epub ahead of print]

pm8Switching cannabinoid response from CB2 agonists to FAAH inhibitors.


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.


CB(2), Cannabinoid, FAAH, IBD, Isoxazoles





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