以间二苯酚为起始原料合成了8种7-羟基黄酮并进行了合成路线的探索,用1HNMR、ESI-MS对化合物进行结构表征,并采用Ellman法测试化合物对乙酰胆碱酯酶(ACh E)和丁酰胆碱酯酶(BCh E)的抑制活性。结果表明,所合成的化合物对ACh E均具有一定的抑制活性,其中,6-甲氧基萘环取代的化合物Ⅲh抑制活性最好,20μmol/L浓度下抑制率为34.71%,优于对照药物卡巴拉汀,为设计治疗阿尔茨海默症药物提供了重要模板。 Eight kinds of 7-hydroxyflavone were synthesized from m-diphenol and the synthetic route was explored. The compounds were characterized by 1HNMR and ESI-MS, and the compounds were tested for their inhibitory effect on acetylcholinesterase (AChE) And butyrylcholinesterase (BCh E). The results showed that the synthesized compounds had certain inhibitory activity against ACh E, of which the compound IIIh substituted with 6-methoxynaphthalene ring had the best inhibitory activity, and the inhibitory rate was 34.71% at the concentration of 20 μmol / L, which was better than that of the control drug Rivastigmine provides an important template for the design of drugs for the treatment of Alzheimer’s disease.