Abstract Six N-glycosyl benzofuran derivatives were synthesized by the catalysis of organic bases and condensation agents. The benzofuran derivatives were obtained by the reaction of various salicylaldehydes in acetone, and then hydrolyzed to the corresponding carboxylic acids. Finally, the target compounds were synthesized by acylation and the reaction conditions were optimized. The acetylcholinesterase (AChE) inhibitory activity of the desired compounds was tested using Ellman’s method. Most of the compounds showed acetylcholinesterase-inhibition activity; N-(2,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)benzofuran-2-carbxamide (5a) showed the best acetylcholinesterase inhibition, with an inhibitory rate of 84%.

中文翻译：

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N-糖基苯并呋喃衍生物的合成及AChE抑制活性

摘要 采用有机碱和缩合剂催化合成了六种N-糖基苯并呋喃衍生物。苯并呋喃衍生物由各种水杨醛在丙酮中反应得到，然后水解成相应的羧酸。最后，通过酰化反应合成目标化合物并优化反应条件。使用 Ellman 方法测试所需化合物的乙酰胆碱酯酶 (AChE) 抑制活性。大多数化合物显示出乙酰胆碱酯酶抑制活性；N-(2,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)benzofuran-2-carbxamide (5a) 对乙酰胆碱酯酶的抑制效果最好，抑制率为 84%。