Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-β aggregation

被引:133
作者
Bolognesi, ML [1 ]
Andrisano, V [1 ]
Bartolini, M [1 ]
Banzi, R [1 ]
Melchiorre, C [1 ]
机构
[1] Univ Bologna, Dept Pharmaceut Sci, Alma Mater Studiorum, I-40126 Bologna, Italy
关键词
D O I
10.1021/jm049156q
中图分类号
R914 [药物化学];
学科分类号
100701 ;
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.
引用
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页码:24 / 27
页数:4
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