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...
Main Authors: | , , , , |
---|---|
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 |
id |
doaj-970ba2fd2a964aac88222406a9542fb6 |
---|---|
record_format |
Article |
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 AT yinlingyun synthesisandbiologicalevaluationof3arylbenzofuranonederivativesaspotentialantialzheimersdiseaseagents AT yuhangmiao synthesisandbiologicalevaluationof3arylbenzofuranonederivativesaspotentialantialzheimersdiseaseagents AT jiesun synthesisandbiologicalevaluationof3arylbenzofuranonederivativesaspotentialantialzheimersdiseaseagents AT xiaojingwang synthesisandbiologicalevaluationof3arylbenzofuranonederivativesaspotentialantialzheimersdiseaseagents |
_version_ |
1721300951172644864 |