Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.
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2019
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Abstract
A series of novel chalcone derivatives was designed, synthesized and evaluated as multifunctional agents for the treatment of AD. Among of these synthesized compounds, compound TM-2 was a selective BuChE inhibitor (IC = 2.6 μM) and selective MAO-B inhibitor (IC = 5.3 μM), which were supported by docking study. Compound TM-2 also showed good antioxidant activity, and was a selective metal chelator, as well as a neuroprotectant. Moreover, compound TM-2 could significantly inhibit self-induced and Cu-induced Aβ aggregation with 70.2% and 80.7% inhibition rate, respectively, and could disaggregate Cu-induced Aβ aggregation (73.5%), the further TEM images observed provided rational explanation. Besides, compound TM-2 displayed good PAMPA-BBB permeability and conformed to the Lipinski's rule of five. Further, compound TM-2 presented precognitive effect on scopolamine-induced memory impairment in vivo assay. Therefore, compound TM-2 might be a promising multifunctional hit compound for the treatment of AD, and the further structure optimization are in progress.
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sang2019designeuropean
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| Authors | Sang, Zhipei;Wang, Keren;Zhang, Pengfei;Shi, Jian;Liu, Wenmin;Tan, Zhenghuai; |
| Journal | European journal of medicinal chemistry |
| Year | 2019 |
| DOI |
S0223-5234(19)30642-7
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