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首页> 外文期刊>Journal of Medicinal Chemistry >Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation
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Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation

机译:丙基多胺配体作为乙酰胆碱酯酶和乙酰胆碱酯酶诱导的淀粉样β聚集的有效抑制剂

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摘要

Heterodimers 4 and 5 were effective inhibitors of acetylcholinesterase (AChE) activity and AChE-induced amyloid-beta (Abeta) aggregation. The peculiar biological profile of 4 can be relevant in studying the molecular basis underlying the nonclassical action of AChE and in addressing the question whether AChE inhibitors can affect the neurotoxic cascade leading to Alzheimer's disease. Compound 4 emerged as the most potent heterodimer so far available to inhibit AChE-induced Abeta aggregation.
机译:异二聚体4和5是乙酰胆碱酯酶(AChE)活性和AChE诱导的淀粉样β(Abeta)聚集的有效抑制剂。 4的特殊生物学特性与研究AChE非经典作用的分子基础以及解决AChE抑制剂是否会影响导致阿尔茨海默氏病的神经毒性级联反应有关。化合物4成为迄今为止可抑制AChE诱导的Abeta聚集的最有效的异二聚体。

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