Author/Authors :
Bandarpalle B. Shankar، نويسنده , , Brian J. Lavey، نويسنده , , Guowei Zhou، نويسنده , , James A. Spitler، نويسنده , , Qiao-ling Tong and for the Jiaxing City Collaborative Project on Neural Tube Defect Prevention، نويسنده , , Razia Rizvi، نويسنده , , De-Yi Yang، نويسنده , , Ronald Wolin، نويسنده , , Joseph A. Kozlowski، نويسنده , , Neng-Yang Shih، نويسنده , , Jie Wu، نويسنده , , R. William Hipkin، نويسنده , , Waldemar Gonsiorek، نويسنده , , Charles A. Lunn، نويسنده ,
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 :
CB2–CB1 receptor ligands , Inverse agonists , cannabinoid receptors , immunomodulatory , anti-inflammatory
