Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents

A series of xanthine derivatives targeting DPP-IV and GPR119 was designed and synthesized through the pharmacophore merging strategy. Systematic optimization of general structure led to the identification of dual modulator 20i with selective DPP-IV inhibition, good GPR119 agonism activity and favorable metabolic stability.195