Chin Chem Lett. 2014, 25:673-6.

Peng-Fei Xiao, Rui Guo, Shao-Qiang Huang , Heng-Jun Cui, Sheng Ye*, Zhiyuan Zhang *

Abstract

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.

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