Author/Authors :
Brian J. Lavey، نويسنده , , Joseph A. Kozlowski، نويسنده , , Bandarpalle B. Shankar، نويسنده , , James M. Spitler، نويسنده , , Guowei Zhou، نويسنده , , De-Yi Yang، نويسنده , , Youheng Shu، نويسنده , , Michael K.C. Wong، نويسنده , , Shing-Chun Wong، نويسنده , , Neng-Yang Shih، نويسنده , , Jie Wu، نويسنده , , Stuart W. McCombie، نويسنده , , Razia Rizvi، نويسنده , , Ronald L. Wolin، نويسنده , , Charles A. Lunn، نويسنده ,
Abstract :
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.
Keywords :
CB2 receptor ligands , cannabinoid receptors , Inverse agonists , Cannabinoid-2 , CB2 , anti-inflammatory
