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Design, Synthesis and Biological Evaluation of Novel Imidazolone Derivatives as Dipeptidyl Peptidase 4 Inhibitors

[ Vol. 9 , Issue. 7 ]


Yang Liu, Chaoyi Jiang, Haoshu Wu, Peng Wu, Meimei Si, Yongzhou Hu and Tao Liu   Pages 938 - 946 ( 9 )


A series of novel imidazolone derivatives were designed and synthesized via a rational drug design strategy. These compounds were obtained from 3-substituted imidazolidine-2,4-dione through alkylation, formylation, dehydration, and amination. The structures were characterized by 1H NMR, 13C NMR, and MS. All target compounds were screened for their DPP-4 inhibitory activity in vitro. The results revealed that some imidazolone derivatives showed potent DPP-4 inhibition. Compound 5b had an IC50 value of 2.21 µM inhibitory activity against DPP-4. As a promising lead compound, compound 5b with DPP-4 binding mode was further studied by docking analysis. The expected interaction mode was obtained.


Diabetes, docking, DPP-4 inhibitors, drug design, imidazolone, synthesis.


ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.

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