新型阿魏酸衍生物的合成、降糖及醛糖还原酶抑制活性

Xianfeng Huang, Yuanyuan Liu, Cheng Zhang, Guoqiang Song
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引用次数: 0

摘要

合成了一类具有尿素基团的新型阿魏酸衍生物,并对其降糖和醛糖还原酶抑制活性进行了评价。几种化合物显示出与商业药物格列本脲相当的体内降糖药。其中,7a和7b的醛糖还原酶抑制活性最强,ic50分别为0.55和3.88 M。通过对接模拟,将化合物7a和12a插入醛糖还原酶活性位点的晶体结构中,确定可能的结合模式。
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Synthesis, hypoglycemic and aldose reductase inhibition activity of novel ferulic acid derivatives
A novel class of ferulic acid derivatives with urea groups were synthesized and evaluated for hypoglycemic and aldose reductase inhibition activities. Several compounds showed comparable in vivo hypoglycemic agents to the commercial drug glibenclamide. Furthermore, of the tested compounds, 7a and 7 b displayed the most potent aldose reductase inhibitory activity in vitro , with an IC 50 of 0.55 and 3.88 M, respectively. Docking simulation was performed to insert compound 7a and 12a into the crystal structure of aldose reductase at active site to determine the probable binding model.
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