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药学学报  2014 

n-酰基-4-苯基噻唑-2-胺类衍生物的设计、合成及其乙酰胆碱酯酶抑制活性的研究

, PP. 813-818

Keywords: n-酰基-4-苯基噻唑-2-胺,乙酰胆碱酯酶抑制剂,阿尔兹海默症

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Abstract:

以α-溴代苯乙酮作为原料,经过3步反应,合成了n-酰基-4-苯基噻唑-2-胺类化合物。采用ellman分光光度法测试了化合物对乙酰胆碱酯酶的体外抑制活性,结果表明,目标化合物具有一定的乙酰胆碱酯酶抑制活性,其中化合物8c的抑制活性最好,其ic50达到了0.51μmol·l-1,优于利斯的明和石杉碱甲。n-酰基-4-苯基噻唑-2-胺对乙酰胆碱酯酶的抑制活性值得进一步研究。

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