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Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids
An anti-neurodegeneration activity study was carried out for 80 flavonoid compounds. The structure–activity analysis of the structures was carried out by performing three different anti-neurodegeneration screening tests, showing that in these structures, the presence of a hydroxy substituent group a...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10609304/ https://www.ncbi.nlm.nih.gov/pubmed/37894669 http://dx.doi.org/10.3390/molecules28207188 |
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author | Preet, Gagan Haj Hasan, Ahlam Ramlagan, Piteesha Fawdar, Shameem Boulle, Fabien Jaspars, Marcel |
author_facet | Preet, Gagan Haj Hasan, Ahlam Ramlagan, Piteesha Fawdar, Shameem Boulle, Fabien Jaspars, Marcel |
author_sort | Preet, Gagan |
collection | PubMed |
description | An anti-neurodegeneration activity study was carried out for 80 flavonoid compounds. The structure–activity analysis of the structures was carried out by performing three different anti-neurodegeneration screening tests, showing that in these structures, the presence of a hydroxy substituent group at position C3′ as well as C5′ of ring B and a methoxy substituent group at the C7 position of ring A play a vital role in neuroprotective and antioxidant as well as anti-inflammatory activity. Further, we found structure (5) was the top-performing active structure out of 80 structures. Subsequently, a molecular docking study was carried out for the 3 lead flavonoid compounds (4), (5), and (23) and 21 similar hypothetical proposed structures to estimate the binding strength between the tested compounds and proteins potentially involved in disease causation. Ligand-based pharmacophores were generated to guide future drug design studies. |
format | Online Article Text |
id | pubmed-10609304 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-106093042023-10-28 Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids Preet, Gagan Haj Hasan, Ahlam Ramlagan, Piteesha Fawdar, Shameem Boulle, Fabien Jaspars, Marcel Molecules Article An anti-neurodegeneration activity study was carried out for 80 flavonoid compounds. The structure–activity analysis of the structures was carried out by performing three different anti-neurodegeneration screening tests, showing that in these structures, the presence of a hydroxy substituent group at position C3′ as well as C5′ of ring B and a methoxy substituent group at the C7 position of ring A play a vital role in neuroprotective and antioxidant as well as anti-inflammatory activity. Further, we found structure (5) was the top-performing active structure out of 80 structures. Subsequently, a molecular docking study was carried out for the 3 lead flavonoid compounds (4), (5), and (23) and 21 similar hypothetical proposed structures to estimate the binding strength between the tested compounds and proteins potentially involved in disease causation. Ligand-based pharmacophores were generated to guide future drug design studies. MDPI 2023-10-20 /pmc/articles/PMC10609304/ /pubmed/37894669 http://dx.doi.org/10.3390/molecules28207188 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Preet, Gagan Haj Hasan, Ahlam Ramlagan, Piteesha Fawdar, Shameem Boulle, Fabien Jaspars, Marcel Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids |
title | Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids |
title_full | Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids |
title_fullStr | Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids |
title_full_unstemmed | Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids |
title_short | Anti-Neurodegenerating Activity: Structure–Activity Relationship Analysis of Flavonoids |
title_sort | anti-neurodegenerating activity: structure–activity relationship analysis of flavonoids |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10609304/ https://www.ncbi.nlm.nih.gov/pubmed/37894669 http://dx.doi.org/10.3390/molecules28207188 |
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