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

Hiroyuki Kai, Yasuhide Morioka, Takami Murashi, Koichi Morita, Satomi Shinonome, Hitoshi Nakazato, Keiko Kawamoto, Kohji Hanasaki, Fumiyo Takahashi, Shin ichi Mihara, Tohko Arai, Kohji Abe, Hiroshi Okabe, Takahiko Baba, Takayoshi Yoshikawa, Hideyuki Takenaka

Research output: Contribution to journalArticlepeer-review

26 Citations (Scopus)

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 CB2 receptor. The most potent compound 13 displays Ki values of >5000 and 9 nM to CB1 and CB2 receptors, respectively.

Original languageEnglish
Pages (from-to)4030-4034
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number14
DOIs
Publication statusPublished - Jul 15 2007
Externally publishedYes

Keywords

  • 1,3-Thiazine
  • CB
  • CB
  • CB receptor selective
  • Cannabinoid receptor agonist
  • Pain
  • Structure-activity relationship

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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