Biaryl cannabinoid mimetics—Synthesis and structure–activity relationship

K Worm, QJ Zhou, GJ Stabley, RN DeHaven…

Index: Worm, Karin; Zhou, Q. Jean; Stabley, Gabriel J.; DeHaven, Robert N.; Dolle, Roland E. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 13 p. 3652 - 3656

Full Text: HTML

Citation Number: 11

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 CB2 receptor agonist.