1489232-55-4Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel imidazolone derivatives as dipeptidyl peptidase 4 inhibitors
Liu, Yang,Jiang, Chaoyi,Wu, Haoshu,Wu, Peng,Si, Meimei,Hu, Yongzhou,Liu, Tao
, p. 938 - 946 (2014/01/06)
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.
