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

Author(s): Yang Liu, Chaoyi Jiang, Haoshu Wu, Peng Wu, Meimei Si, Yongzhou Hu, Tao Liu

Journal Name: Medicinal Chemistry

Volume 9 , Issue 7 , 2013

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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.

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

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Article Details

Year: 2013
Page: [938 - 946]
Pages: 9
DOI: 10.2174/1573406411309070007
Price: $65

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