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OALib Journal期刊
ISSN: 2333-9721
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新型[1,3]二氧杂环戊烯并[4,5-f]异吲哚酮衍生物的设计、合成与活性研究
, PP. 191-198
Keywords: [1,3]二氧杂环戊烯并[4,5-f]异吲哚酮,乙酰胆碱酯酶抑制剂,记忆障碍,阿尔茨海默症
Abstract:
本文设计、合成了一系列新型[1,3]二氧杂环戊烯并[4,5-f]异吲哚酮衍生物,并对其进行了乙酰胆碱酯酶抑制活性以及由东莨菪碱致小鼠记忆障碍的改善作用测试。实验结果表明目标化合物对乙酰胆碱酯酶(ache)均有抑制作用,ic50值在微摩尔级,其中化合物i1(ic50=0.086μmol·l-1)和i2(ic50=0.080μmol·l-1)对ache的抑制活性较好,与阳性药多奈哌齐(ic50=0.094μmol·l-1)相当;且化合物i1～i4均具有改善由东莨菪碱引起的小鼠记忆障碍的作用。
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