Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Sağlık, Begüm Nurpelin, Levent, Serkan, Osmaniye, Derya, Evren, Asaf Evrim, Karaduman, Abdullah Burak, Özkay, Yusuf, Kaplancıklı, Zafer Asım
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
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
_version_ 1784855396325785600
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
work_keys_str_mv AT saglıkbegumnurpelin designsynthesisandinvitroandinsilicoapproachesofnovelindanonederivativesasmultifunctionalantialzheimeragents
AT leventserkan designsynthesisandinvitroandinsilicoapproachesofnovelindanonederivativesasmultifunctionalantialzheimeragents
AT osmaniyederya designsynthesisandinvitroandinsilicoapproachesofnovelindanonederivativesasmultifunctionalantialzheimeragents
AT evrenasafevrim designsynthesisandinvitroandinsilicoapproachesofnovelindanonederivativesasmultifunctionalantialzheimeragents
AT karadumanabdullahburak designsynthesisandinvitroandinsilicoapproachesofnovelindanonederivativesasmultifunctionalantialzheimeragents
AT ozkayyusuf designsynthesisandinvitroandinsilicoapproachesofnovelindanonederivativesasmultifunctionalantialzheimeragents
AT kaplancıklızaferasım designsynthesisandinvitroandinsilicoapproachesofnovelindanonederivativesasmultifunctionalantialzheimeragents