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Synthesis, physical-chemical characterisation and biological evaluation of novel 2-amido-3-hydroxypyridin-4(1H)-ones: Iron chelators with the potential for treating Alzheimer's disease

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Synthesis, physical-chemical characterisation and biological evaluation of novel 2-amido-3-hydroxypyridin-4(1H)-ones: Iron chelators with the potential for treating Alzheimer's disease. / Gaeta, Alessandra; Molina-Holgado, Francisco; Kong, Xiao L.; Salvage, Sarah; Fakih, Sarah; Francis, Paul T.; Williams, Robert J.; Hider, Robert C.

In: Bioorganic and Medicinal Chemistry, Vol. 19, No. 3, 01.02.2011, p. 1285 - 1297.

Research output: Contribution to journalArticle

Harvard

Gaeta, A, Molina-Holgado, F, Kong, XL, Salvage, S, Fakih, S, Francis, PT, Williams, RJ & Hider, RC 2011, 'Synthesis, physical-chemical characterisation and biological evaluation of novel 2-amido-3-hydroxypyridin-4(1H)-ones: Iron chelators with the potential for treating Alzheimer's disease', Bioorganic and Medicinal Chemistry, vol. 19, no. 3, pp. 1285 - 1297. https://doi.org/10.1016/j.bmc.2010.12.007

APA

Gaeta, A., Molina-Holgado, F., Kong, X. L., Salvage, S., Fakih, S., Francis, P. T., ... Hider, R. C. (2011). Synthesis, physical-chemical characterisation and biological evaluation of novel 2-amido-3-hydroxypyridin-4(1H)-ones: Iron chelators with the potential for treating Alzheimer's disease. Bioorganic and Medicinal Chemistry, 19(3), 1285 - 1297. https://doi.org/10.1016/j.bmc.2010.12.007

Vancouver

Gaeta A, Molina-Holgado F, Kong XL, Salvage S, Fakih S, Francis PT et al. Synthesis, physical-chemical characterisation and biological evaluation of novel 2-amido-3-hydroxypyridin-4(1H)-ones: Iron chelators with the potential for treating Alzheimer's disease. Bioorganic and Medicinal Chemistry. 2011 Feb 1;19(3):1285 - 1297. https://doi.org/10.1016/j.bmc.2010.12.007

Author

Gaeta, Alessandra ; Molina-Holgado, Francisco ; Kong, Xiao L. ; Salvage, Sarah ; Fakih, Sarah ; Francis, Paul T. ; Williams, Robert J. ; Hider, Robert C. / Synthesis, physical-chemical characterisation and biological evaluation of novel 2-amido-3-hydroxypyridin-4(1H)-ones: Iron chelators with the potential for treating Alzheimer's disease. In: Bioorganic and Medicinal Chemistry. 2011 ; Vol. 19, No. 3. pp. 1285 - 1297.

Bibtex Download

@article{9595c518c83845a0b567d7d54be01128,
title = "Synthesis, physical-chemical characterisation and biological evaluation of novel 2-amido-3-hydroxypyridin-4(1H)-ones: Iron chelators with the potential for treating Alzheimer's disease",
abstract = "A novel class of 2-amido-3-hydroxypyridin-4-one iron chelators is described. These compounds have been designed to behave as suitable molecular probes which will improve our knowledge of the role of iron in neurodegenerative conditions. Neurodegenerative disorders, such as Alzheimer's disease (AD) and Parkinson disease (PD), can be considered as diverse pathological conditions sharing critical metabolic processes such as protein aggregation and oxidative stress. Interestingly, both these metabolic alterations seem to be associated with the involvement of metal ions, including iron. Iron chelation is therefore a potential therapeutic approach. The physico-chemical (pK(a) pFe(3+) and log P) and biological properties (inhibition of iron-containing enzymes) of these chelators have been investigated in order to obtain a suitable profile for the treatment of neurodegenerative conditions. Studies with neuronal cell cultures confirm that the new iron chelators are neuroprotective against beta-amyloid-induced toxicity. (C) 2010 Elsevier Ltd. All rights reserved.",
author = "Alessandra Gaeta and Francisco Molina-Holgado and Kong, {Xiao L.} and Sarah Salvage and Sarah Fakih and Francis, {Paul T.} and Williams, {Robert J.} and Hider, {Robert C.}",
year = "2011",
month = "2",
day = "1",
doi = "10.1016/j.bmc.2010.12.007",
language = "English",
volume = "19",
pages = "1285 -- 1297",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
publisher = "Elsevier Limited",
number = "3",

}

RIS (suitable for import to EndNote) Download

TY - JOUR

T1 - Synthesis, physical-chemical characterisation and biological evaluation of novel 2-amido-3-hydroxypyridin-4(1H)-ones: Iron chelators with the potential for treating Alzheimer's disease

AU - Gaeta, Alessandra

AU - Molina-Holgado, Francisco

AU - Kong, Xiao L.

AU - Salvage, Sarah

AU - Fakih, Sarah

AU - Francis, Paul T.

AU - Williams, Robert J.

AU - Hider, Robert C.

PY - 2011/2/1

Y1 - 2011/2/1

N2 - A novel class of 2-amido-3-hydroxypyridin-4-one iron chelators is described. These compounds have been designed to behave as suitable molecular probes which will improve our knowledge of the role of iron in neurodegenerative conditions. Neurodegenerative disorders, such as Alzheimer's disease (AD) and Parkinson disease (PD), can be considered as diverse pathological conditions sharing critical metabolic processes such as protein aggregation and oxidative stress. Interestingly, both these metabolic alterations seem to be associated with the involvement of metal ions, including iron. Iron chelation is therefore a potential therapeutic approach. The physico-chemical (pK(a) pFe(3+) and log P) and biological properties (inhibition of iron-containing enzymes) of these chelators have been investigated in order to obtain a suitable profile for the treatment of neurodegenerative conditions. Studies with neuronal cell cultures confirm that the new iron chelators are neuroprotective against beta-amyloid-induced toxicity. (C) 2010 Elsevier Ltd. All rights reserved.

AB - A novel class of 2-amido-3-hydroxypyridin-4-one iron chelators is described. These compounds have been designed to behave as suitable molecular probes which will improve our knowledge of the role of iron in neurodegenerative conditions. Neurodegenerative disorders, such as Alzheimer's disease (AD) and Parkinson disease (PD), can be considered as diverse pathological conditions sharing critical metabolic processes such as protein aggregation and oxidative stress. Interestingly, both these metabolic alterations seem to be associated with the involvement of metal ions, including iron. Iron chelation is therefore a potential therapeutic approach. The physico-chemical (pK(a) pFe(3+) and log P) and biological properties (inhibition of iron-containing enzymes) of these chelators have been investigated in order to obtain a suitable profile for the treatment of neurodegenerative conditions. Studies with neuronal cell cultures confirm that the new iron chelators are neuroprotective against beta-amyloid-induced toxicity. (C) 2010 Elsevier Ltd. All rights reserved.

U2 - 10.1016/j.bmc.2010.12.007

DO - 10.1016/j.bmc.2010.12.007

M3 - Article

VL - 19

SP - 1285

EP - 1297

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

SN - 0968-0896

IS - 3

ER -

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