title: 2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 2: orally bioavailable compounds.
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.
authors.affiliation: Shionogi Research Laboratories, Shionogi & Co. Ltd, 12-4, Sagisu 5-chome, Osaka 553-0002, Japan. hiroyuki.kai@shionogi.co.jp
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Kai
authors.forename: Yasuhide
authors.initials: Y
authors.lastname: Morioka
authors.forename: Minoru
authors.initials: M
authors.lastname: Tomida
authors.forename: Tadashi
authors.initials: T
authors.lastname: Takahashi
authors.forename: Maki
authors.initials: M
authors.lastname: Hattori
authors.forename: Kohji
authors.initials: K
authors.lastname: Hanasaki
authors.forename: Katsumi
authors.initials: K
authors.lastname: Koike
authors.forename: Hiroki
authors.initials: H
authors.lastname: Chiba
authors.forename: Shunji
authors.initials: S
authors.lastname: Shinohara
authors.forename: Toshiyuki
authors.initials: T
authors.lastname: Kanemasa
authors.forename: Yuka
authors.initials: Y
authors.lastname: Iwamoto
authors.forename: Kohji
authors.initials: K
authors.lastname: Takahashi
authors.forename: Yoshitaka
authors.initials: Y
authors.lastname: Yamaguchi
authors.forename: Takahiko
authors.initials: T
authors.lastname: Baba
authors.forename: Takayoshi
authors.initials: T
authors.lastname: Yoshikawa
authors.forename: Hideyuki
authors.initials: H
authors.lastname: Takenaka
mesh_terms: D000284:Administration, Oral; D001682:Biological Availability; D063386:Cannabinoid Receptor Agonists; D013843:Thiazines / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D063386:Cannabinoid Receptor Agonists; D013843:Thiazines