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Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitors
Alzheimer’s disease (AD) is a neuroinflammatory based pathologic state in which β-amyloid aggregates are major devastating agents. In this study, a series of 2-hydroxyiminoethanones were synthesized and evaluated as anti-inflammatory in carrageenan and formalin tests and inhibitors of β-amyloid aggr...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Shaheed Beheshti University of Medical Sciences
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6934981/ https://www.ncbi.nlm.nih.gov/pubmed/32641939 http://dx.doi.org/10.22037/ijpr.2019.15567.13181 |
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author | Valipour, Mehdi Davaji, Issa Abedi, Niusha Rajabi, Mahsa Küçükkılınç, Tuba Tüylü Ayazgök, Beyza Irannejad, Hamid |
author_facet | Valipour, Mehdi Davaji, Issa Abedi, Niusha Rajabi, Mahsa Küçükkılınç, Tuba Tüylü Ayazgök, Beyza Irannejad, Hamid |
author_sort | Valipour, Mehdi |
collection | PubMed |
description | Alzheimer’s disease (AD) is a neuroinflammatory based pathologic state in which β-amyloid aggregates are major devastating agents. In this study, a series of 2-hydroxyiminoethanones were synthesized and evaluated as anti-inflammatory in carrageenan and formalin tests and inhibitors of β-amyloid aggregation. Compounds 1-10b were synthesized through a two-step reaction. Results: Compounds 1-5b showed more β-amyloid disaggregation ability than reference drugs rifampicin and donepezil and compound 2b was the best compound in this series and could reduce the extent of amyloid aggregation to 50.9%. Interestingly, compounds 1b and 3b showed significant anti-inflammatory activity in carrageenan-induced paw edema compared to control group and equivalent to the reference drug indomethacin. 2-Hydeoxyiminoethanones are privileged scaffold for further drug research and development as anti-neuroinflammatory and neuroprotective agents. |
format | Online Article Text |
id | pubmed-6934981 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Shaheed Beheshti University of Medical Sciences |
record_format | MEDLINE/PubMed |
spelling | pubmed-69349812020-07-07 Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitors Valipour, Mehdi Davaji, Issa Abedi, Niusha Rajabi, Mahsa Küçükkılınç, Tuba Tüylü Ayazgök, Beyza Irannejad, Hamid Iran J Pharm Res Original Article Alzheimer’s disease (AD) is a neuroinflammatory based pathologic state in which β-amyloid aggregates are major devastating agents. In this study, a series of 2-hydroxyiminoethanones were synthesized and evaluated as anti-inflammatory in carrageenan and formalin tests and inhibitors of β-amyloid aggregation. Compounds 1-10b were synthesized through a two-step reaction. Results: Compounds 1-5b showed more β-amyloid disaggregation ability than reference drugs rifampicin and donepezil and compound 2b was the best compound in this series and could reduce the extent of amyloid aggregation to 50.9%. Interestingly, compounds 1b and 3b showed significant anti-inflammatory activity in carrageenan-induced paw edema compared to control group and equivalent to the reference drug indomethacin. 2-Hydeoxyiminoethanones are privileged scaffold for further drug research and development as anti-neuroinflammatory and neuroprotective agents. Shaheed Beheshti University of Medical Sciences 2019 /pmc/articles/PMC6934981/ /pubmed/32641939 http://dx.doi.org/10.22037/ijpr.2019.15567.13181 Text en This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Original Article Valipour, Mehdi Davaji, Issa Abedi, Niusha Rajabi, Mahsa Küçükkılınç, Tuba Tüylü Ayazgök, Beyza Irannejad, Hamid Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitors |
title | Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitors |
title_full | Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitors |
title_fullStr | Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitors |
title_full_unstemmed | Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitors |
title_short | Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitors |
title_sort | synthesis and biological assessment of 2-hydroxyiminoethanones as anti-inflammatory and β-amyloid aggregation inhibitors |
topic | Original Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6934981/ https://www.ncbi.nlm.nih.gov/pubmed/32641939 http://dx.doi.org/10.22037/ijpr.2019.15567.13181 |
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