摘要
背景：根据流行病学研究，假设死亡率，有效预防措施，确定性诊断指南或治愈性治疗没有变化，患有痴呆症的人数将每20年增加近一倍，到2030年为6570万，2050年为1.154亿。从上述流行病学数据可以看出，痴呆症不仅在目前，而且在将来也是一个重大的公共卫生问题。 目的和方法：Pomponi等人在1997年已经合成了几种N-烷基化他克林（THA）衍生物。然而，使用从Electrophorus electricus分离的酶测试了这些化合物的抗AChE活性。出于这个原因，我们决定扩展先前报道的THA衍生物系列，并因此在实验电池中进行测试，其结果从阿尔兹美病的角度对这些化合物进行了更为相关的评估。由庞波尼出版。 结果和结论：总之，所有感兴趣的化合物在体外有效抑制ChEs。具有N-辛基链的最有希望的衍生物之一显示出与他克林相比高出2.5倍的AChE抑制活性。关于血脑屏障（BBB）渗透，可以声称合成的类似物可能能够穿过BBB。从肝毒性的观点来看，与他克林相比，选择的N-烷基化他克林衍生物产生更差的结果。然而，体外结果仅是说明性的，因此，只有体内实验才能确定所选N-烷基化THA衍生物的实际价值。
关键词: 他克林，阿尔茨海默病，乙酰胆碱酯酶，丁酰胆碱酯酶，痴呆，神经。
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