Title of article :
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 2: Orally bioavailable compounds
Author/Authors :
Hiroyuki Kai، نويسنده , , Yasuhide Morioka، نويسنده , , Minoru Tomida، نويسنده , , and Tadashi Takahashi، نويسنده , , Maki Hattori، نويسنده , , Kohji Hanasaki، نويسنده , , Katsumi Koike، نويسنده , , Hiroki Chiba، نويسنده , , Shunji Shinohara، نويسنده , , Toshiyuki Kanemasa، نويسنده , , Yuka Iwamoto، نويسنده , , Kohji Takahashi، نويسنده , , Yoshitaka Yamaguchi، نويسنده , , Takahiko Baba، نويسنده , , Takayoshi Yoshikawa، نويسنده , , Hideyuki Takenaka، نويسنده ,
Abstract :
Structure–activity relationships and efforts to optimize the pharmacokinetic profile of a class of 2-arylimino-5,6-dihydro-4H-1,3-thiazines as cannabinoid receptor agonists are described. Among the compounds examined, compound 14 showed potent affinity and high selectivity for CB2, and compound 23 showed potent affinities against CB1 and CB2. These compounds displayed oral bioavailability.
