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Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies
Authors:Shankar Bandarpalle B  Lavey Brian J  Zhou Guowei  Spitler James A  Tong Ling  Rizvi Razia  Yang De-Yi  Wolin Ronald  Kozlowski Joseph A  Shih Neng-Yang  Wu Jie  Hipkin R William  Gonsiorek Waldemar  Lunn Charles A
Affiliation:Department of Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA. bandarpalle.shankar@spcorp.com
Abstract:We recently reported that compound 1 is a potent inhibitor of the CB2 receptor with high selectivity over CB1. This paper describes the SAR development for this class of compounds. Variation of the substitution pattern on the aromatic rings, as well as the groups linking them together, led to sub-nanomolar inhibitors of the CB2 receptor, with high selectivity over CB1.
Keywords:
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