title: 2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: discovery of CB2 receptor selective compounds.
abstract: 2-Arylimino-5,6-dihydro-4H-1,3-thiazines have been identified as a novel class of cannabinoid agonists. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure-activity relationships led to the discovery of potent agonists of CB(2) receptor. The most potent compound 13 displays K(i) values of >5000 and 9 nM to CB(1) and CB(2) receptors, respectively.
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: Takami
authors.initials: T
authors.lastname: Murashi
authors.forename: Koichi
authors.initials: K
authors.lastname: Morita
authors.forename: Satomi
authors.initials: S
authors.lastname: Shinonome
authors.forename: Hitoshi
authors.initials: H
authors.lastname: Nakazato
authors.forename: Keiko
authors.initials: K
authors.lastname: Kawamoto
authors.forename: Kohji
authors.initials: K
authors.lastname: Hanasaki
authors.forename: Fumiyo
authors.initials: F
authors.lastname: Takahashi
authors.forename: Shin-ichi
authors.initials: S
authors.lastname: Mihara
authors.forename: Tohko
authors.initials: T
authors.lastname: Arai
authors.forename: Kohji
authors.initials: K
authors.lastname: Abe
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Okabe
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: D000818:Animals; D063386:Cannabinoid Receptor Agonists; D051381:Rats; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D063386:Cannabinoid Receptor Agonists; D013843:Thiazines