Expansion of SAR studies on triaryl bis sulfone cannabinoid CB2 receptor ligands

Ling Tong, B B Shankar, Lei Chen, Razia Rizvi, Joseph Kelly, Eric Gilbert, Chunli Huang, De-Yi Yang, Joseph A Kozlowski, N-Y Shih, W Gonsiorek, R William Hipkin, Asra Malikzay, Charles A Lunn, Daniel J Lundell
Bioorganic & Medicinal Chemistry Letters 2010 November 15, 20 (22): 6785-9
We report further expansion of the structure activity relationship (SAR) on the triaryl bis sulfone class of compounds (I), which are potent CB(2) receptor ligands with excellent selectivity over the CB(1) receptor. This study was extended to B ring changes, followed by simultaneous optimization of the A-, B-, and C-rings. Compound 42 has excellent CB(2) potency, selectivity and rat exposure.

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