Biaryl cannabinoid mimetics—Synthesis and structure–activity relationship

Synthesis, in vitro biological evaluation, and structure–activity relationships of a biaryl cannabinoid mimetic 2 are reported. Variations in the substitution pattern yielded a number of agonists with low nanomolar affinity. Replacing the phenol group by a methyl morpholino acetate group led to compound 28, a 500-fold selective CB2 receptor agonist.

Graphical abstractA series of novel-substituted biaryl cannabinoid mimetics was synthesized and their biological activity determined.Figure optionsDownload full-size imageDownload as PowerPoint slide