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

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.

Graphical abstractAmong the 2-arylimino-5,6dihydro-4H-1,3-thiazines, the most potent compound 13 displays Ki values of >5000 and 9 nM to CB1 and CB2 receptors, respectively.Figure optionsDownload full-size imageDownload as PowerPoint slide