2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: Discovery of CB₂ receptor selective compounds

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• 作者：Hiroyuki Kai ; Yasuhide Morioka ; Takami Murashi ; Koichi Morita ; Satomi Shinonome ; Hitoshi Nakazato ; Keiko Kawamoto ; Kohji Hanasaki ; Fumiyo Takahashi ; Shin-ichi Mihara ; et al.
• 关键词：1 ; 3-Thiazine ; Cannabinoid receptor agonist ; CB₂ receptor selective ; CB₁ ; CB₂ ; Pain ; Structure– ; activity relationship
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 出版时间：15 July 2007
• 年：2007
• 卷：17
• 期：14
• 页码：4030-4034
• 全文大小：193 K

文摘

2-Arylimino-5,6-dihydro-4H-1,3-thiazines have been identified as a novel class of cannabinoid agonists. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure–activity relationships led to the discovery of potent agonists of CB₂ receptor. The most potent compound 13 displays K_i values of >5000 and 9 nM to CB₁ and CB₂ receptors, respectively.