【摘要】 利用Dakin-West反应"一锅法"合成了12个N-{[（硫色满-4-酮-3-基）-苯基]-甲基}乙酰胺衍生物。所合成的化合物经¹H NMR、¹³C NMR、IR和HR-MS等方法进行了结构表征。葡萄糖氧化酶法测试结果表明,大多数目标分子表现出α-葡萄糖苷酶抑制活性,其中化合物4k抑制作用最强(在浓度为5.39 mmol·L^-1时,绝对抑制活性达到87.3%)。根据活性测试结果对合成化合物的构效关系进行了讨论。用分子对接方法研究了化合物4k与α-葡萄糖苷酶的作用模式,为进一步的研究提供了依据。更多还原

【Abstract】 In order to develop potent antidiabetic agents that have inhibitory effect to α-glucosidase, twelve β-acetamido ketone derivatives such as N-{[（substituted-4-oxo-thiochroman-3-yl）phenyl]-methyl}acetamide are designed and synthesized through one-pot Dakin-West reaction. Their chemical structures are confirmed by ¹H NMR, ¹³ C NMR, IR and HR-MS. In vitro α-glucosidase inhibition assays of compounds 4a-4l were carried out using glucose oxidase method. The result indicated that most of them possess inhibitory activity in vitro. Compound 4k showed the most potent inhibitory activity with 87.3% inhibition of α-glucosidase at the concentration of 5.39 mmol·L^-1. The structure-activity relationship of these β-acetamido ketone derivatives was discussed preliminarily. Moreover, the molecular docking method was used to study the interaction mode of compound 4k and α-glucosidase. Our results will be helpful for designing of α-glucosidase inhibitors in the future.更多还原