- Design, synthesis, and physicochemical and biological characterization of a new iron chelator of the family of hydroxychromenes
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Increasing evidence suggests that iron plays an important role in tissue damage both during chronic iron overload diseases (i.e., hemochromatosis) and when, in the absence of actual tissue iron overload, iron is delocalized from specific carriers or intracellular sites (inflammation, neurodegenerative diseases, postischaemic reperfusion, xenobiotic intoxications, etc.). In the present work, we appropriately modified an iron chelator of the hydroxychromene family in order to obtain a tridentate chelator that would inactivate the iron redox cycle after its complexation, with a view to using this molecule in human therapy and/or in disease prevention. We synthesized such a chelator for the first time and show, by different physicochemical analysis, its tridentate nature and, importantly, its capacity to chelate iron with enough strength to inhibit both iron-dependent H2O2 generation and lipid peroxidation in in vitro biological systems.
- Ferrali, Marco,Bambagioni, Sabrina,Ceccanti, Antonio,Donati, Donato,Giorgi, Giancola,Fontani, Marco,Laschi, Franco,Zanello, Piero,Casolaro, Mario,Pietrangelou, Antonello
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- Aromatic derivatives and iron complexes thereof for the use as normalizing agents of the iron level
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The present invention is directed to aromatic derivatives of formula (I), wherein: R1is (a), wherein R3and R4are selected from between H and OH, provided that R3and R4are not simultaneously H, and R2is H; or R1and R2taken together, are (b), wherein R5is selected from between CH3and (CH2)5OH, to the iron complexes thereof, and to their use for the preparation of pharmaceutical compositions for the normalization of iron level.
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