Synthesis and biological evaluation of 2-arylbenzofuran derivatives as potential anti-Alzheimer’s disease agents
| Autor: | Xiao-Jing Wang, Yuhang Miao, Sun Xiaoya, Jie Sun, Yinling Yun |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
Drug
cholinesterase inhibitors media_common.quotation_subject RM1-950 Pharmacology 01 natural sciences chemistry.chemical_compound Alzheimer Disease Drug Discovery medicine Humans Donepezil IC50 Nootropic Agents 2-Arylbenzofuran derivatives Benzofurans Cholinesterase media_common biology β-secretase inhibitory activity 010405 organic chemistry Chemistry General Medicine Alzheimer's disease Acetylcholinesterase In vitro 0104 chemical sciences Baicalein 010404 medicinal & biomolecular chemistry Toxicity biology.protein Therapeutics. Pharmacology Research Article Research Paper medicine.drug |
| Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry article-version (VoR) Version of Record Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 1345-1355 (2021) |
| ISSN: | 1475-6374 1475-6366 |
| DOI: | 10.1080/14756366.2021.1940993 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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