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

Bioorg Med Chem Lett. 2007 Jul 15;17(14):4030-4. doi: 10.1016/j.bmcl.2007.04.093. Epub 2007 Apr 30.


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.

MeSH terms

  • Animals
  • Cannabinoid Receptor Agonists*
  • Rats
  • Structure-Activity Relationship
  • Thiazines / chemistry
  • Thiazines / pharmacokinetics
  • Thiazines / pharmacology*


  • Cannabinoid Receptor Agonists
  • Thiazines