7-羟基黄酮的合成及活性

Synthesis and Biological Evaluation of 7-Hydroxyflavones

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 7-hydroxyflavones were synthesized and their strcutures were confirmed by1 HNMR and ESI-MS. Their acetylcholinesterase（ ACh E） and butyrylcholinesterase（ BCh E） inhibitory activities was determined by the Ellman method. The result showed that the synthesized compounds had potent ACh E inhibitory activity at 20 μmol / L,compound Ⅲh displayed the most potent ACh E inhibition（ 34. 71%）,which was slight better than Rivastigmine. The results indicate that these 7-hydroxyflavones may provide a useful template for the development of anti-AD agents.