Dipeptidyl peptidase Ⅳ（DPP4） inhibitors are proven in the treatment of type 2 diabetes.We designed and synthesized a series of novel indole compounds that selectively inhibit the activity of DPP4 over dipeptidyl pe...Dipeptidyl peptidase Ⅳ（DPP4） inhibitors are proven in the treatment of type 2 diabetes.We designed and synthesized a series of novel indole compounds that selectively inhibit the activity of DPP4 over dipeptidyl peptidase 9（DPP9）（〉200 fold）.We further co-crystallized DPP4 with indole sulfonamide（compound 1） to confirm a proposed binding mode.Good metabolic stability of the indole compounds represents another positive attribute for further development.展开更多
基金supported in part by funds from the Ministry of Science and Technology (No. 2014CB910300)the Natural Science Foundation of Zhejiang Province (No. R2100439)the Specialized Research Fund for the Doctoral Program of Higher Education (No. 20110101110122)
文摘Dipeptidyl peptidase Ⅳ（DPP4） inhibitors are proven in the treatment of type 2 diabetes.We designed and synthesized a series of novel indole compounds that selectively inhibit the activity of DPP4 over dipeptidyl peptidase 9（DPP9）（〉200 fold）.We further co-crystallized DPP4 with indole sulfonamide（compound 1） to confirm a proposed binding mode.Good metabolic stability of the indole compounds represents another positive attribute for further development.
