2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: Discovery of CB sub(2) receptor selective compounds

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 sub(2) receptor. Th...

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Published inBioorganic & medicinal chemistry letters Vol. 17; no. 14; pp. 4030 - 4034
Main Authors Kai, Hiroyuki, Morioka, Yasuhide, Murashi, Takami, Morita, Koichi, Shinonome, Satomi, Nakazato, Hitoshi, Kawamoto, Keiko, Hanasaki, Kohji, Takahashi, Fumiyo, Mihara, Shin-Ichi, Arai, Tohko, Abe, Kohji, Okabe, Hiroshi, Baba, Takahiko, Yoshikawa, Takayoshi, Takenaka, Hideyuki
Format Journal Article
LanguageEnglish
Published 01.07.2007
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Summary: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 sub(2) receptor. The most potent compound 13 displays K sub(i) values of >5000 and 9 nM to CB sub(1) and CB sub(2) receptors, respectively.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.04.093