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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.
We designed and synthesized a series of novel indole compounds that produced inhibitory 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.