Inhibitors of dipeptidyl peptidase-4 (DPP4) have been shown to be effective treatments for type 2 diabetes. A series of novel 1,2,3-triazole based xanthine derivatives were designed and evaluated for in vitro dipeptidyl peptidase-4 (DPP-4) activity. Among them, the representative compounds 7b, 7e, 7g and 6eshowed excellent inhibitory activity of DPP-4 with IC50 values ranging from 87.41 to 16.34 nM, respectively. The SAR of these xanthine derivatives have been discussed, which would be useful for developing novel DPP-4 inhibitors as treating type 2 diabetes
