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Design, Synthesis, and In Vitro and In Silico Approaches of Novel Indanone Derivatives as Multifunctional Anti-Alzheimer Agents
[Image: see text] Alzheimer’s disease (AD) is a neurological, progressive illness that typically affects the elderly and is clinically distinguished by memory and cognitive decline. Due to a number of factors, including the absence of a radical treatment, an increase in the patient population over t...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2022
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9774391/ https://www.ncbi.nlm.nih.gov/pubmed/36570177 http://dx.doi.org/10.1021/acsomega.2c06906 |
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author | Sağlık, Begüm Nurpelin Levent, Serkan Osmaniye, Derya Evren, Asaf Evrim Karaduman, Abdullah Burak Özkay, Yusuf Kaplancıklı, Zafer Asım |
author_facet | Sağlık, Begüm Nurpelin Levent, Serkan Osmaniye, Derya Evren, Asaf Evrim Karaduman, Abdullah Burak Özkay, Yusuf Kaplancıklı, Zafer Asım |
author_sort | Sağlık, Begüm Nurpelin |
collection | PubMed |
description | [Image: see text] Alzheimer’s disease (AD) is a neurological, progressive illness that typically affects the elderly and is clinically distinguished by memory and cognitive decline. Due to a number of factors, including the absence of a radical treatment, an increase in the patient population over time, the high cost of care and treatment, and a significant decline in patients’ quality of life, the importance of this disease has increased. These factors have all prompted increased interest among researchers in this field. The chemical structure of the donepezil molecule, the most popular and effective treatment response for AD, served as the basis for the design and synthesis of 42 novel indan-1-one derivatives in this study. Using IR, (1)H, and (13)C NMR as well as mass spectroscopic techniques, the compounds’ structures were identified. Research on the compounds’ antioxidant activities, cholinesterase (ChE) enzyme inhibition, monoamine oxidase (MAO) A and B inhibitory activities, β-amyloid plaque inhibition, and cytotoxicity impact was carried out. Inhibition of β-amyloid plaque aggregation; effective inhibition of AChE, BChE, and MAO-B enzymes; and significant antioxidant activity were all demonstrated by compounds D28–D30 and D37–D39. Because of their various actions, it was hypothesized that the related compounds may be useful in treating AD symptoms as well as providing palliative care. |
format | Online Article Text |
id | pubmed-9774391 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-97743912022-12-23 Design, Synthesis, and In Vitro and In Silico Approaches of Novel Indanone Derivatives as Multifunctional Anti-Alzheimer Agents Sağlık, Begüm Nurpelin Levent, Serkan Osmaniye, Derya Evren, Asaf Evrim Karaduman, Abdullah Burak Özkay, Yusuf Kaplancıklı, Zafer Asım ACS Omega [Image: see text] Alzheimer’s disease (AD) is a neurological, progressive illness that typically affects the elderly and is clinically distinguished by memory and cognitive decline. Due to a number of factors, including the absence of a radical treatment, an increase in the patient population over time, the high cost of care and treatment, and a significant decline in patients’ quality of life, the importance of this disease has increased. These factors have all prompted increased interest among researchers in this field. The chemical structure of the donepezil molecule, the most popular and effective treatment response for AD, served as the basis for the design and synthesis of 42 novel indan-1-one derivatives in this study. Using IR, (1)H, and (13)C NMR as well as mass spectroscopic techniques, the compounds’ structures were identified. Research on the compounds’ antioxidant activities, cholinesterase (ChE) enzyme inhibition, monoamine oxidase (MAO) A and B inhibitory activities, β-amyloid plaque inhibition, and cytotoxicity impact was carried out. Inhibition of β-amyloid plaque aggregation; effective inhibition of AChE, BChE, and MAO-B enzymes; and significant antioxidant activity were all demonstrated by compounds D28–D30 and D37–D39. Because of their various actions, it was hypothesized that the related compounds may be useful in treating AD symptoms as well as providing palliative care. American Chemical Society 2022-12-07 /pmc/articles/PMC9774391/ /pubmed/36570177 http://dx.doi.org/10.1021/acsomega.2c06906 Text en © 2022 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by/4.0/Permits the broadest form of re-use including for commercial purposes, provided that author attribution and integrity are maintained (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Sağlık, Begüm Nurpelin Levent, Serkan Osmaniye, Derya Evren, Asaf Evrim Karaduman, Abdullah Burak Özkay, Yusuf Kaplancıklı, Zafer Asım Design, Synthesis, and In Vitro and In Silico Approaches of Novel Indanone Derivatives as Multifunctional Anti-Alzheimer Agents |
title | Design, Synthesis,
and In Vitro and In Silico Approaches
of Novel Indanone Derivatives as Multifunctional
Anti-Alzheimer Agents |
title_full | Design, Synthesis,
and In Vitro and In Silico Approaches
of Novel Indanone Derivatives as Multifunctional
Anti-Alzheimer Agents |
title_fullStr | Design, Synthesis,
and In Vitro and In Silico Approaches
of Novel Indanone Derivatives as Multifunctional
Anti-Alzheimer Agents |
title_full_unstemmed | Design, Synthesis,
and In Vitro and In Silico Approaches
of Novel Indanone Derivatives as Multifunctional
Anti-Alzheimer Agents |
title_short | Design, Synthesis,
and In Vitro and In Silico Approaches
of Novel Indanone Derivatives as Multifunctional
Anti-Alzheimer Agents |
title_sort | design, synthesis,
and in vitro and in silico approaches
of novel indanone derivatives as multifunctional
anti-alzheimer agents |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9774391/ https://www.ncbi.nlm.nih.gov/pubmed/36570177 http://dx.doi.org/10.1021/acsomega.2c06906 |
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