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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. 2008
Hiroyuki Kai, and
Yasuhide Morioka, and
Yuji Koriyama, and
Kazuya Okamoto, and
Yasushi Hasegawa, and
Maki Hattori, and
Katsumi Koike, and
Hiroki Chiba, and
Shunji Shinohara, and
Yuka Iwamoto, and
Kohji Takahashi, and
Norihiko Tanimoto
Shionogi Research Laboratories, Shionogi & Co., Ltd, 12-4, Sagisu 5-chome, Fukushima-ku, Osaka 553-0002, Japan. hiroyuki.kai@shionogi.co.jp
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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