Title: Discovery of dipeptidyl peptidase IV (DPP4) inhibitors based on a novel indole scaffold Xiao P, Guo R, Huang S, Cui H, Ye S, Zhang Z Ref: Chin Chem Lett, 25:673, 2014 : PubMed
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.
