349141-25-9Relevant articles and documents
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.
experimental part, p. 1285 - 1297 (2011/03/23)
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 (pKa, 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 β-amyloid-induced toxicity.
IRON MODULATORS
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Page/Page column 12; Figure 2, (2010/11/24)
Iron modulator compounds of formula (I) are provided for treating amyloidoses wherein R1 is selected from H, C1-6 alkyl, C1-6 alkenyl, C1-6 hydroxyalkyl, C1-6 hydroxyalkenyl, R2 is selected from H, C1-6 alkyl, C1-6 alkenyl, C1-6 hydroxyalkyl, C1-6 hydroxyalkenyl and C6-10 aralykyl in which the aryl group of the aralkyl group is optionally substituted by hydroxy, halo or C1-4 alkyl R3 is selected from H, C1-6 alkyl, C1-6 alkenyl and C1-12 acyl; R4 is selected from H and C1-3 alkyl R5, R6 and R7 are independently selected from H, C1-6 alkyl, C3-7 aryl, and C1-10 aralkyl; the alkyl, aryl and aralkyl groups being optionally substituted by one or more halo, hydroxy and nitro groups or R5 and R7 together with the nitrogen atom to which they are bonded form a heterocyclic ring optionally substituted by one or more hydroxyl groups or a pharmaceutically acceptable tautomer, ester or addition salt thereof.
Novel synthetic approach to 2-(1′-hydroxyalkyl)- and 2-amido-3-hydroxypyridin-4-ones
Piyamongkol, Sirivipa,Liu, Zu D,Hider, Robert C
, p. 3479 - 3486 (2007/10/03)
Novel methods for the synthesis of high pFe3+ iron chelators, 2-(1′-hydroxyalkyl)- and 2-amido-3-hydroxypyridin-4-ones, have been developed. The products are obtained, via N-oxide intermediates, from either maltol or ethyl maltol.
