transfusion-dependent patients such as those suffering from β-thalassaemia develop a fatal secondary haemosiderosis and consequently a selective iron chelator must be used to relieve such iron overload. 3- hydroxypyridin-4-ones are selective for iron(iii) under most biological conditions, but unlike desferrioxamine, are efficiently absorbed when administered orally. in this study, the synthesis...

iron overload is a serious clinical condition which can be largely prevented by the use of iron-specific chelating agents. in this study, the synthesis and determination of partition coefficients (kpart) of a range of n-alkyl hydroxypyridinones, as orally active iron chelators, are described. synthesis of n-aryl hydroxypyridinones was achieved via a single step synthetic pathway. in this method...

transfusion in the treatment of thalassemia gives rise to iron deposits in many organs. since there are many obstacles in the use of deferoxamin (dfo) as an iron chelating agent, it is important to find another alternative therapy that can act as iron chelation. the study aims to compare the histopathological pictures of the heart and spleen in iron-induced rats after administration of dfo and ...

Current iron chelation therapy consists primarily of DFO (desferrioxamine), which has to be administered via intravenous infusion, together with deferiprone and deferasirox, which are orally-active chelators. These chelators, although effective at decreasing the iron load, are associated with a number of side effects. Grady suggested that the combined administration of a smaller bidentate chela...

objectives: iron chelators, such as maltol and kojic acid, have antioxidant and anti-inflammatory properties. they may have beneficial effects on inflammatory bowel disease (ibd) because iron can develop and aggravate inflammation in ibd. in the present study, the effect of selected iron chelators and anti-oxidants were evaluated on a model of trinitrobenzene sulfonic acid (tnbs)-induced coliti...

A series of bidentate hydroxypyridinone iron chelators that have therapeutic potential as oral iron chelators, have been studied systematically to determine which properties are the most critical for the mobilization of hepatocyte iron. The relationship between lipid solubility of the free and complexed forms of each chelator and hepatocyte iron release has been investigated as well as the cont...

utilized iron chelator produced a dramatic effect on survival of patients with thalassemia. However, DFO has poor oral bioavailability and a short half life, necessitating 12 hours of subcutaneous infusion, rendering therapy extremely cumbersome [1]. Deferiprone (DFP), an orally effective iron chelator, reduces total body iron load and is also effective in removing cardiac iron [1-3]. However, ...

The membrane associated iron chelator of Pseudomonas aeruginosa has been extracted from membranes of iron-rich cells with ethanol and purified by reverse phase HPLC. Using 13C NMR and FAB mass spectroscopy, the structure of the chelator has been determined to be 4-hydroxy-2-nonylquinoline. This compound has been previously isolated and named pseudan IX, a name which we use here. We synthesized ...

ICL670(deferasirox) is a tridentate oral iron chelator that has shown high efficacy and theraputic safety in preclinical and currently ongoing phase III clinical evaluation. The drug has been just approved by US FDA for use in iron-loading anaemias. It is an ideal once-daily oral chelator, the effective dose of which is between 20 and 40 mg/kg. Iron is chelated & excreted almost exclusively via...