Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands

Brian J Lavey, Joseph A Kozlowski, Bandarpalle B Shankar, James M Spitler, Guowei Zhou, De-Yi Yang, Youheng Shu, Michael K C Wong, Shing-Chun Wong, Neng-Yang Shih, Jie Wu, Stuart W McCombie, Razia Rizvi, Ronald L Wolin, Charles A Lunn
Bioorganic & Medicinal Chemistry Letters 2007 July 1, 17 (13): 3760-4
Structure-activity relationship on our recently reported triaryl bis-sulfone class of cannabinoid-2 (CB2) receptor selective inverse agonists was explored. Modifications to the methane sulfonamide, substitutions to B and C phenyl rings, and replacements of the C-ring were investigated. A compound with excellent CB2 activity, selectivity for CB2 over CB1, and in vivo plasma levels was identified.

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