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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、~(13)C 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。
Twelve N - {[(thiochroman-4-one-3-yl) -phenyl] -methyl} acetamide derivatives were synthesized by the Dakin-West reaction. The synthesized compounds were characterized by ~ 1H NMR, ~ (13) C NMR, IR and HR-MS. The results of glucose oxidase test showed that most of the target molecules exhibited α-glucosidase inhibitory activity, of which compound 4k had the strongest inhibitory effect (at a concentration of 5.39 mmol·L -1, the absolute inhibitory activity reached 87.3% ). The structure-activity relationship of the synthesized compounds is discussed according to the activity test results. The mode of interaction between 4k and α-glucosidase was studied by molecular docking method, which provided the basis for further research.