2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 3: Synthesis and activity of isosteric analogs |
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Authors: | Kai Hiroyuki Morioka Yasuhide Koriyama Yuji Okamoto Kazuya Hasegawa Yasushi Hattori Maki Koike Katsumi Chiba Hiroki Shinohara Shunji Iwamoto Yuka Takahashi Kohji Tanimoto Norihiko |
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Institution: | Shionogi Research Laboratories, Shionogi & Co., Ltd, 12-4, Sagisu 5-chome, Fukushima-ku, Osaka 553-0002, Japan. hiroyuki.kai@shionogi.co.jp |
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Abstract: | Structure-activity relationships and efforts to optimize the pharmacokinetic profile of isosteric analogs of 2-arylimino-5,6-dihydro-4H-1,3-thiazines as cannabinoid receptor agonists are described. Among those examined, compound 25 showed potent affinity for cannabinoid receptor 1 (CB1) and receptor 2 (CB2). This compound displayed oral bioavailability and analgesic activity. |
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