Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands
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- 作者：Brian J. Lavey ; Joseph A. Kozlowski ; B ; arpalle B. Shankar ; James M. Spitler ; Guowei Zhou ; De-Yi Yang ; Youheng Shu ; Michael K.C. Wong ; Shing-Chun Wong ; Neng-Yang Shih ; et al.
- 关键词：CB2 receptor ligands ; Inverse agonists ; Cannabinoid receptors ; Cannabinoid-2 ; CB2 ; Anti-inflammatory
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：1 July 2007
- 年：2007
- 卷：17
- 期：13
- 页码：3760-3764
- 全文大小：165 K
文摘
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.