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Development of the “hidden” multi-target-directed ligands by AChE/BuChE for the treatment of Alzheimer's disease by Rui Chen; Xinjuan Li; Hongsong Chen; Keren Wang; Teng Xue; Jing Mi; Yujuan Ban; Gaofeng Zhu; Yi Zhou; Wu Dong; Lei Tang; Zhipei Sang is a Chemistry article available to read on EtoBox.
What is Development of the “hidden” multi-target-directed ligands by AChE/BuChE for the treatment of Alzheimer's disease about?
Accumulation of evidences suggested that excessive amounts of AChE and BuChE in the brain of AD patients at the different stage of AD, which could hydrolyze ACh and accelerated Aβ aggregation. To develop new “hidden” multifunctional agents through AChE/BuChE would be a promising strategy to treat AD. To this end, firstly, a series of chalcone derivatives with chelating property was designed and synthesized. The in vitro results showed that compound 3f indicated significant selective MAO-B inhibitory activity (IC50 = 0.67 μM) and remarkable anti-inflammatory property. It also significantly inhibited self-induced Aβ 1-42 aggregation and showed remarkable neuroprotective effects on Aβ 25-35-induced PC12 cell injury. Furthermore, compound 3f was a selective metal chelator and could inhibit Cu2+-induced Aβ 1-42 aggregation. Based on this, the carbamate fragment was introduced to compound 3f to obtain carbamate derivatives. The biological activity results exhibited that compound 4b showed good BBB permeability, good AChE inhibitory potency (IC50 = 5.3 μM), moderate BuChE inhibitory potency (IC50 = 12.4 μM), significant MAO-B inhibitory potency, anti-inflammation potency on LPS-induced BV
Who reads Development of the “hidden” multi-target-directed ligands by AChE/BuChE for the treatment of Alzheimer's disease?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Rui Chen; Xinjuan Li; Hongsong Chen; Keren Wang; Teng Xue; Jing Mi; Yujuan Ban; Gaofeng Zhu; Yi Zhou; Wu Dong; Lei Tang; Zhipei Sang
- Publisher
- Elsevier BV
- Published
- 2023
- Language
- EN
- Field
- Chemistry (Physical Sciences)