Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer’s disease agents

Multi-target drugs can better address the cascade of events involved in oxidative stress and the reduction in cholinergic transmission that occur in Alzheimer’s disease than cholinesterase inhibitors alone. We synthesised a series of 3-arylbenzofuranone derivatives and evaluated their antioxidant ac...

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Main Authors: Jie Yang, Yinling Yun, Yuhang Miao, Jie Sun, Xiaojing Wang
Format: Article
Language:English
Published: Taylor & Francis Group 2020-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
Online Access:http://dx.doi.org/10.1080/14756366.2020.1740694
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spelling doaj-970ba2fd2a964aac88222406a9542fb62021-07-15T13:10:32ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742020-01-0135180581410.1080/14756366.2020.17406941740694Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer’s disease agentsJie Yang0Yinling Yun1Yuhang Miao2Jie Sun3Xiaojing Wang4School of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical SciencesSchool of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical SciencesSchool of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical SciencesInstitute of Materia Medica, Shandong First Medical University and Shandong Academy of Medical SciencesInstitute of Materia Medica, Shandong First Medical University and Shandong Academy of Medical SciencesMulti-target drugs can better address the cascade of events involved in oxidative stress and the reduction in cholinergic transmission that occur in Alzheimer’s disease than cholinesterase inhibitors alone. We synthesised a series of 3-arylbenzofuranone derivatives and evaluated their antioxidant activity, cholinesterase inhibitory activity, and monoamine oxidase inhibitory activity. 3-Arylbenzofuranone compounds exhibit good antioxidant activity as well as selective acetylcholinesterase inhibitory activity. The IC50 value of anti-acetylcholinesterase inhibition of Compound 20 (0.089 ± 0.01 μM) is similar to the positive drug donepezil (0.059 ± 0.003 μM). According to the experimental results, Compounds 7, 13 show a certain effect in the in vitro evaluation performed and have the potential as drug candidates for the treatment of Alzheimer’s disease.http://dx.doi.org/10.1080/14756366.2020.17406943-arylbenzofuranone derivativesalzheimer’s diseasecholinesterase inhibitorsmonoamine oxidase inhibitorsantioxidant activity
collection DOAJ
language English
format Article
sources DOAJ
author Jie Yang
Yinling Yun
Yuhang Miao
Jie Sun
Xiaojing Wang
spellingShingle Jie Yang
Yinling Yun
Yuhang Miao
Jie Sun
Xiaojing Wang
Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer’s disease agents
Journal of Enzyme Inhibition and Medicinal Chemistry
3-arylbenzofuranone derivatives
alzheimer’s disease
cholinesterase inhibitors
monoamine oxidase inhibitors
antioxidant activity
author_facet Jie Yang
Yinling Yun
Yuhang Miao
Jie Sun
Xiaojing Wang
author_sort Jie Yang
title Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer’s disease agents
title_short Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer’s disease agents
title_full Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer’s disease agents
title_fullStr Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer’s disease agents
title_full_unstemmed Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer’s disease agents
title_sort synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-alzheimer’s disease agents
publisher Taylor & Francis Group
series Journal of Enzyme Inhibition and Medicinal Chemistry
issn 1475-6366
1475-6374
publishDate 2020-01-01
description Multi-target drugs can better address the cascade of events involved in oxidative stress and the reduction in cholinergic transmission that occur in Alzheimer’s disease than cholinesterase inhibitors alone. We synthesised a series of 3-arylbenzofuranone derivatives and evaluated their antioxidant activity, cholinesterase inhibitory activity, and monoamine oxidase inhibitory activity. 3-Arylbenzofuranone compounds exhibit good antioxidant activity as well as selective acetylcholinesterase inhibitory activity. The IC50 value of anti-acetylcholinesterase inhibition of Compound 20 (0.089 ± 0.01 μM) is similar to the positive drug donepezil (0.059 ± 0.003 μM). According to the experimental results, Compounds 7, 13 show a certain effect in the in vitro evaluation performed and have the potential as drug candidates for the treatment of Alzheimer’s disease.
topic 3-arylbenzofuranone derivatives
alzheimer’s disease
cholinesterase inhibitors
monoamine oxidase inhibitors
antioxidant activity
url http://dx.doi.org/10.1080/14756366.2020.1740694
work_keys_str_mv AT jieyang synthesisandbiologicalevaluationof3arylbenzofuranonederivativesaspotentialantialzheimersdiseaseagents
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