期刊
MOLECULAR DIVERSITY
卷 22, 期 4, 页码 841-861出版社
SPRINGER
DOI: 10.1007/s11030-018-9835-2
关键词
Synthesis; In vitro; alpha-glucosidase; Structure-activity relationship (SAR); In silico
类别
资金
- Higher Education Commission (HEC) Pakistan under the National Research Program for Universities [20-1910]
This study is focused on the identification of thiazole-based inhibitors for the alpha-glucosidase enzyme. For that purpose, (E)-2-(2-(arylmethylene) hydrazinyl)-4-arylthiazole derivatives were synthesized in two steps and characterized by various spectroscopic techniques. All derivatives and intermediates were evaluated for their in vitro alpha-glucosidase inhibitory activity. Thiosemicarbazones 20 and 35, and cyclized thiazole derivatives 2, 5-11, 13, 15, 21-24, 27-31, and 36-37 showed significant inhibitory potential in the range of IC50 = 6.2 +/- 0.19-43.6 +/- 0.23 mu M as compared to standard acarbose (IC50 = 37.7 +/- 0.19 mu M). A molecular modeling study was carried out to understand the binding interactions of compounds with the active site of enzyme.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据