Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors

Bioorganic & Medicinal Chemistry Letters
Ning LiDa-Yong Shi

Abstract

A series of novel pyrimidinedione derivatives were designed and evaluated for in vitro dipeptidyl peptidase-4 (DPP-4) inhibitory activity and in vivo anti-hyperglycemic efficacy. Among them, the representative compounds 11, 15 and 16 showed excellent inhibitory activity of DPP-4 with IC50 values of 64.47 nM, 188.7 nM and 65.36 nM, respectively. Further studies revealed that compound 11 was potent in vivo hypoglycemic effect. The structure-activity relationships of these pyrimidinedione derivatives had been discussed, which would be useful for developing novel DPP-4 inhibitors as treating type 2 diabetes.

Citations

Jun 18, 2019·Expert Opinion on Therapeutic Patents·Hidayat HussainIftikhar Ali
Feb 6, 2020·Bioorganic & Medicinal Chemistry·Jayanta Dowarah, Ved Prakash Singh
Aug 25, 2021·Bioorganic & Medicinal Chemistry·Shubham KumarAmit Mittal

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