| Literature DB >> 27810241 |
Guangcheng Wang1, Zhiyun Peng2, Jing Wang2, Juan Li2, Xin Li2.
Abstract
A novel series of 2,4,5-triarylimidazole-1,2,3-triazole derivatives were synthesized via copper(I)-catalyzed azide-alkyne click chemistry, and evaluated for their α-glucosidase inhibitory activity. All tested compounds showed potent α-glucosidase inhibitory activity with IC50 ranging from 15.16±0.18 to 48.15±0.37μM, in comparison to the standard drug, acarbose (IC50=817.38±6.27μM). Among all the tested compounds, 5j was found to be the most active compound with IC50 value of 15.16±0.18μM and behaved as a noncompetitive inhibitor with a Ki of 14.78μM. In addition, molecular docking study was carried out to explore the binding interactions of these compounds with α-glucosidase enzyme.Entities:
Keywords: 1,2,3-Triazole; 2,4,5-Triarylimidazole; Click chemistry; Enzyme kinetic study; Molecular docking; α-Glucosidase inhibitor
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Year: 2016 PMID: 27810241 DOI: 10.1016/j.bmcl.2016.10.057
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823