| Literature DB >> 28189421 |
Guangcheng Wang1, Xin Li2, Jing Wang2, Zhenzhen Xie2, Luyao Li2, Ming Chen2, Shan Chen2, Yaping Peng2.
Abstract
A novel series of 2-((5,6-diphenyl-1,2,4-triazin-3-yl)thio)-N-arylacetamides 5a-5q have been synthesized and evaluated for their α-glucosidase inhibitory activity. All newly synthesized compounds exhibited potent α-glucosidase inhibitory activity in the range of IC50=12.46±0.13-72.68±0.20μM, when compared to the standard drug acarbose (IC50=817.38±6.27μM). Among the series, compound 5j (12.46±0.13μM) with strong electron-withdrawing nitro group on the arylacetamide moiety was identified as the most potent inhibitor of α-glucosidase. Molecular docking study was carried out to explore the binding interactions of these compounds with α-glucosidase. Our study identifies a novel series of potent α-glucosidase inhibitors for further investigation.Entities:
Keywords: 1,2,4-Triazine; Molecular docking; α-Glucosidase inhibitor
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Year: 2017 PMID: 28189421 DOI: 10.1016/j.bmcl.2017.01.094
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823