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

Hiroyuki Kai; Yasuhide Morioka; Takami Murashi; Koichi Morita; Satomi Shinonome; Hitoshi Nakazato; Keiko Kawamoto; Kohji Hanasaki; Fumiyo Takahashi; Shin ichi Mihara; Tohko Arai; Kohji Abe; Hiroshi Okabe; Takahiko Baba; Takayoshi Yoshikawa; Hideyuki Takenaka

doi:10.1016/j.bmcl.2007.04.093

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

Hiroyuki Kai, Yasuhide Morioka, Takami Murashi, Koichi Morita, Satomi Shinonome, Hitoshi Nakazato, Keiko Kawamoto, Kohji Hanasaki, Fumiyo Takahashi, Shin ichi Mihara, Tohko Arai, Kohji Abe, Hiroshi Okabe, Takahiko Baba, Takayoshi Yoshikawa, Hideyuki Takenaka

研究成果 › 査読

30 被引用数 (Scopus)

抄録

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.

本文言語	English
ページ（範囲）	4030-4034
ページ数	5
ジャーナル	Bioorganic and Medicinal Chemistry Letters
巻	17
号	14
DOI	https://doi.org/10.1016/j.bmcl.2007.04.093
出版ステータス	Published - 7月 15 2007
外部発表	はい

ASJC Scopus subject areas

生化学
分子医療
分子生物学
薬科学
創薬
臨床生化学
有機化学

文献へのアクセス

10.1016/j.bmcl.2007.04.093

他のファイルとリンク

フィンガープリント

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引用スタイル

Kai, H., Morioka, Y., Murashi, T., Morita, K., Shinonome, S., Nakazato, H., Kawamoto, K., Hanasaki, K., Takahashi, F., Mihara, S. I., Arai, T., Abe, K., Okabe, H., Baba, T., Yoshikawa, T., & Takenaka, H. (2007). 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. Bioorganic and Medicinal Chemistry Letters, 17(14), 4030-4034. https://doi.org/10.1016/j.bmcl.2007.04.093

Kai, H, Morioka, Y, Murashi, T, Morita, K, Shinonome, S, Nakazato, H, Kawamoto, K, Hanasaki, K, Takahashi, F, Mihara, SI, Arai, T, Abe, K, Okabe, H, Baba, T, Yoshikawa, T & Takenaka, H 2007, '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', Bioorganic and Medicinal Chemistry Letters, vol. 17, no. 14, pp. 4030-4034. https://doi.org/10.1016/j.bmcl.2007.04.093

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