The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives

Benzimidazolone derivatives were discovered as novel CB2 selective agonists. Structure Activity Relationship (SAR) studies around them were examined to improve metabolic stability. Compound 39 exhibited excellent metabolic stability in human liver microsomes (HLM) and significant attenuation of the chronic colonic allodynia in the TNBS-treated rats by po administration.

Benzimidazolone derivatives as novel CB2 selective agonists are reported. Compound 39 exhibited excellent metabolic stability and significant attenuation of the visceral allodynia in a rat model by oral administration.Figure optionsDownload as PowerPoint slide