Biaryl cannabinoid mimetics--synthesis and structure-activity relationship |
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Authors: | Worm Karin Zhou Q Jean Stabley Gabriel J DeHaven Robert N Dolle Roland E |
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Affiliation: | Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA, USA. kworm@adolor.com |
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Abstract: | 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 CB(2) receptor agonist. |
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