Title of article :
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
Author/Authors :
Hiroyuki Kai، نويسنده , , Yasuhide Morioka، نويسنده , , Yuji Koriyama، نويسنده , , Kazuya Okamoto، نويسنده , , Yasushi Hasegawa، نويسنده , , Maki Hattori، نويسنده , , Katsumi Koike، نويسنده , , Hiroki Chiba، نويسنده , , Shunji Shinohara، نويسنده , , Yuka Iwamoto، نويسنده , , Kohji Takahashi، نويسنده , , Norihiko Tanimoto، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
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.
Keywords :
CB2 , Oral bioavailability , Cannabinoid receptor agonist , analgesic activity , 3-Thiazine , 1 , Isosteric analog , 3-Oxazine , 1 , CB1
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters