Non-aromatic A-ring replacement in the triaryl bis-sulfone CB2 receptor inhibitors
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- 作者：Eric J. Gilbert ; Guowei Zhou ; Michael K.C. Wong ; Ling Tong ; B ; arpalle B. Shankar ; Chunli Huang ; Joseph Kelly ; Brian J. Lavey ; Stuart W. McCombie ; Lei Chen ; Razia Rizvi ; Youhao Dong ; Youheng Shu ; Josep
- 关键词：CB2 ; Cannabinoid ; Inverse agonist
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 January 2010
- 年：2010
- 卷：20
- 期：2
- 页码：608-611
- 全文大小：1066 K
文摘
The triaryl bis-sulfone 1 was modified by converting the aryl A-ring to a piperidine ring. The piperidine ring was further elaborated to a spirocyclopropyl piperidine moiety. The effect on CB2 binding potency, rat calcium channel affinity, and CYP 2C9 inhibition is described.