Synthesis and biological evaluation of 2-arylbenzofuran derivatives as potential anti-Alzheimer’s disease agents |
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Authors: | Yinling Yun Yuhang Miao Xiaoya Sun Jie Sun Xiaojing Wang |
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Affiliation: | Institute of Materia Medica, Shandong First Medical University and Shandong Academy of Medical Sciences, Jinan, China |
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Abstract: | Alzheimer''s disease (AD) is a type of progressive dementia caused by degeneration of the nervous system. A single target drug usually does not work well. Therefore, multi-target drugs are designed and developed so that one drug can specifically bind to multiple targets to ensure clinical effectiveness and reduce toxicity. We synthesised a series of 2-arylbenzofuran derivatives and evaluated their in vitro activities. 2-Arylbenzofuran compounds have good dual cholinesterase inhibitory activity and β-secretase inhibitory activity. The IC50 value of compound 20 against acetylcholinesterase inhibition (0.086 ± 0.01 µmol·L−1) is similar to donepezil (0.085 ± 0.01 µmol·L−1) and is better than baicalein (0.404 ± 0.04 µmol·L−1). And most of the compounds have good BACE1 inhibitory activity, of which 3 compounds (8, 19 and 20) show better activity than baicalein (0.087 ± 0.03 µmol·L−1). According to experimental results, 2-arylbenzofuran compounds provide an idea for drug design to develop prevention and treatment for AD. |
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Keywords: | 2-Arylbenzofuran derivatives, Alzheimer''s disease, cholinesterase inhibitors, β -secretase inhibitory activity |
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