基于多靶点药物设计策略,以染料木素为先导化合物,对其7-位和4’-位羟基进行修饰,合成了24个染料木素氨基甲酸酯类衍生物,其化学结构经1HNMR和HRMS确证.生物活性测试结果表明,部分化合物对乙酰胆碱酯酶具有较强抑制活性,且对H202诱导的PCI2细胞氧化损伤具有显著保护作用.
With genistein as lead compound, twenty-four genistein carbamate derivatives were synthesized from genistein with the structural modification of 7-OH and 4'-OH based on the muti-target-directed drug design strategy. The chemical structures of target compounds were confirmed by 1H NMR and HRMS techniques. Their acetylcholinesterase and butylcho- linesterase inhibitory activity and neuroprotective effects against hydrogen peroxide induced PC12 cell injury were evaluated in vitro. The results indicated that some compounds exhibited the most potent acetylcholinesterase inhibitory activity and neuroprotective effects.