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Synthesis and Evaluation of Paeonol Derivatives as Potential Multifunctional Agents for the Treatment of Alzheimer’s Disease

1
Institute of Natural Medicine, Hefei University of Technology, Hefei 230009, Anhui, China
2
Anhui Province Key Laboratory of R&D of Chinese Medicine, Anhui University of Chinese Medicine, Hefei 230038, Anhui, China
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Derek J. McPhee
Molecules 2015, 20(1), 1304-1318; https://doi.org/10.3390/molecules20011304
Received: 10 November 2014 / Accepted: 7 January 2015 / Published: 14 January 2015
(This article belongs to the Section Organic Chemistry)
Alzheimer’s disease (AD) is a progressive neurodegenerative brain disorder characterized by memory loss, language impairment, personality changes and intellectual decline. Taking into account the key pathological features of AD, such as low levels of acetylcholine, beta-amyloid (Aβ) aggregation, oxidative stress and dyshomeostasis of biometals, a new series of paeonol derivatives 5a5d merging three different functions, i.e., antioxidant, anti-acetylcholinesterase (AChE) activity, metal chelating agents for AD treatment have been synthesized and characterized. Biological assays revealed that compared with paeonol (309.7 μM), 5a5d had a lower DPPH IC50 value (142.8–191.6 μM). 5a5d could significantly inhibit hydrogen peroxide-induced neuronal PC12 cell death assessed by MTT assay in the concentration range of 5–40 μM. AChE activity was effectively inhibited by 5a5d, with IC50 values in the range of 0.61–7.04 μM. 5a5d also exhibited good metal-chelating ability. All the above results suggested that paeonol derivatives may be promising multifunctional agents for AD treatment. View Full-Text
Keywords: Alzheimer’s disease; multifunctional agents; paeonol; acetylcholinesterase inhibitors; metal-chelating; biometal chelators Alzheimer’s disease; multifunctional agents; paeonol; acetylcholinesterase inhibitors; metal-chelating; biometal chelators
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Zhou, A.; Wu, H.; Pan, J.; Wang, X.; Li, J.; Wu, Z.; Hui, A. Synthesis and Evaluation of Paeonol Derivatives as Potential Multifunctional Agents for the Treatment of Alzheimer’s Disease. Molecules 2015, 20, 1304-1318.

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