Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands
BJ Lavey, JA Kozlowski, BB Shankar, JM Spitler…
文献索引：Lavey, Brian J.; Kozlowski, Joseph A.; Shankar, Bandarpalle B.; Spitler, James M.; Zhou, Guowei; Yang, De-Yi; Shu, Youheng; Wong, Michael K.C.; Wong, Shing-Chun; Shih, Neng-Yang; Wu, Jie; McCombie, Stuart W.; Rizvi, Razia; Wolin, Ronald L.; Lunn, Charles A. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 13 p. 3760 - 3764
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.
