Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.

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2019
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Abstract
A series of novel chalcone-O-alkylamine derivatives were designed, synthesized and evaluated as multifunctional anti-Alzheimer's disease agents. Based on the experimental results, compound 23c exhibited good inhibitory potency on both acetylcholinesterase (IC = 1.3 ± 0.01 μM) and butyrylcholinesterase (IC = 1.2 ± 0.09 μM). Besides, 23c exhibited selective MAO-B inhibitory activity with IC value of 0.57 ± 0.01 μM. Compound 23c was also a potential antioxidant and neuroprotectant. In addition, compound 23c could inhibit self-induced Aβ aggregation. Moreover, compound 23c was a selective metal chelator, and could inhibit and disaggregate Cu-induced Aβ aggregation, which was supported by the further transmission electron microscopy images. Furthermore, 23c could cross the blood-brain barrier in vitro, and improved scopolamine-induced memory impairment in vivo assay. Molecular modeling studies showed that 23c could bind to the active site of AChE, BuChE, Aβ and MAO-B. Taken together, these results suggested that compound 23c might be a potential multifunctional agent for the treatment of AD.
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bai2019developmenteuropean Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Bai, Ping;Wang, Keren;Zhang, Pengfei;Shi, Jian;Cheng, Xinfeng;Zhang, Qi;Zheng, Cheng;Cheng, Yao;Yang, Jian;Lu, Xiaoxia;Sang, Zhipei;
Journal European journal of medicinal chemistry
Year 2019
DOI
S0223-5234(19)30889-X
URL
Keywords
synthesis alzheimer's disease rational design chalcone-o-alkylamine derivatives multi-functional agents precognitive effect

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