中文摘要：

以硫磺素T为母体,合成和表征了一种解聚金属-Aβ聚集体的荧光螯合剂5-氨基-2-（苯并[d]噻唑-2-基）苯酚（FC-9）,研究了它与金属-Aβ聚集体的相互作用以及由此导致的Aβ聚集体的构象、形貌和毒性变化。结果表明,FC-9不仅能识别各种Aβ40/Aβ42聚集体,而且还能使金属-Aβ40/42聚集体解聚。FC-9与金属-Aβ聚集体相互作用后,聚集体的形貌由纤维状转化为无定形状,其β-折叠构象也减少了。FC-9还能够跨过细胞膜,符合严格的Lipinski类药标准,在一定程度上可抑制由Cu-Aβ40聚集体产生的毒性,这使得FC-9在螯合治疗老年痴呆症方面可能具有潜在的应用前景。

英文摘要：

A thioflavin T-based fluorescent chelator 5-amino-2-（benzo[d]thiazol-2-yl）phenol （FC-9） was synthesized and characterized. Its interaction with metal-Aβ aggregates and the change of morphology, conformation, cytotoxicity of the resulting Aβ aggregates were investigated. The results showed that FC-9 can not only recognize different Aβ40/Aβ42 aggregates but also disaggregate metal-Aβ40/Aβ42 aggregates. After the interaction between FC-9 and metal-Aβ40/Aβ42 aggregates, the morphology of aggregates changed from fibril to amorphousness, and their β-sheet conformation was also reduced. Moreover, the cell membrane penetration of FC- 9 fulfilled common drug-like criteria, and it can inhibit cytotoxicity of the Cu-Aβ40 aggregates, indicating that it could have potential prospect in the treatment of Alzheimer disease. CCDC： 960540.