| Title : Discovery of dipeptidyl peptidase IV (DPP4) inhibitors based on a novel indole scaffold - Xiao_2014_Chin.Chem.Lett_25_673 |
| Author(s) : Xiao P , Guo R , Huang S , Cui H , Ye S , Zhang Z |
| Ref : Chin Chem Lett , 25 :673 , 2014 |
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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. |
| PubMedSearch : Xiao_2014_Chin.Chem.Lett_25_673 |
| PubMedID: |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | Indolesufonamide1 |
| Gene_locus | human-DPP4 |
| Structure | 4PV7 |
Xiao P, Guo R, Huang S, Cui H, Ye S, Zhang Z (2014)
Discovery of dipeptidyl peptidase IV (DPP4) inhibitors based on a novel indole scaffold
Chin Chem Lett
25 :673
Xiao P, Guo R, Huang S, Cui H, Ye S, Zhang Z (2014)
Chin Chem Lett
25 :673