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

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

Volume: 9 Issue: 7

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Liu Yang, Jiang Chaoyi, Wu Haoshu, Wu Peng, Si Meimei, Hu Yongzhou and Liu Tao, Design, Synthesis and Biological Evaluation of Novel Imidazolone Derivatives as Dipeptidyl Peptidase 4 Inhibitors, Medicinal Chemistry 2013; 9 (7) . https://dx.doi.org/10.2174/1573406411309070007