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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...

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Autores principales: Valipour, Mehdi, Davaji, Issa, Abedi, Niusha, Rajabi, Mahsa, Küçükkılınç, Tuba Tüylü, Ayazgök, Beyza, Irannejad, Hamid
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2019
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.
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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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