The synthesis and physicochemical properties of a range of 2- and 6-amido-3-hydroxypyridin-4-ones are described. All the amido-substituted 3-hydroxypyridin-4-ones have lower pK(a) values than 1,2-dimethyl-3-hydroxypyridin-4-one (deferiprone). This is due to the inductive effect of the amido group. Furthermore, the pK(a) values of the 3-hydroxy group in 1-nonsubstituted pyridinones are dramatica...

The complex-forming ability of 2-methyl-3-hydroxypyran-4-one (1a), 2-ethyl-3-hydroxypyran-4-one (1b), 1,2-dimethyl-3-hydroxypyridin-4-one (4a) and 1-ethyl-2-methyl-3-hydroxypyridin-4-one (4b) with nickel(Ni(II)) were characterized by infrared, ultraviolet, proton nuclear magnetic resonance spectroscopy and melting point. The mole-ratio of nickel:ligands was analyzed by atomic-absorption-spectro...

the complex-forming ability of 2-methyl-3-hydroxypyran-4-one ( 1a ), 2-ethyl-3-hydroxypyran-4-one ( 1b ), 1,2-dimethyl-3-hydroxypyridin-4-one ( 4a ) and 1-ethyl-2-methyl-3-hydroxypyridin-4-one ( 4b ) with nickel(ni(ii)) were characterized by infrared, ultraviolet, proton nuclear magnetic resonance spectroscopy and melting point. the mole-ratio of nickel:ligands was analyzed by atomic-absorption...

The mechanism of in vivo iron chelation by 3-hydroxypyridin-4-ones (CP compounds) was studied in hypertransfused rats in which the major storage iron pools in hepatocytes and in the reticuloendothelial (RE) system have been labeled by selective radioiron probes. Both dimethyl-3-hydroxypyridin-4-one (CP 20 or L1) and diethyl-3-hydroxypyridine-4-one (CP 94) have an identical and very high (log be...

Seasonal and pandemic influenza outbreaks remain a major human health problem. Inhibition of the endonuclease activity of influenza RNA-dependent RNA polymerase is attractive for the development of new agents for the treatment of influenza infection. Our earlier studies identified a series of 5- and 6-phenyl substituted 3-hydroxypyridin-2(1H)-ones that were effective inhibitors of influenza end...

Recently, it has been shown that a number of hydroxypyridinones such as 1,2-dimethyl-3-hydroxypyridin-4-one (L1) are useful for the treatment of iron overload in place of desferrioxamine in thalassaemic patients. In this study, the intestinal absorption (I.A.) of L1 and one of its analogues namely 2-methy-3-hydroxypyridin-4-one (L2), which possesses a higher partition coefficient (Kpart) than L...

Recently, it has been shown that a number of hydroxypyridinones such as 1,2-dimethyl-3-hydroxypyridin-4-one (L1) are useful for the treatment of iron overload in place of desferrioxamine in thalassaemic patients. In this study, the intestinal absorption (I.A.) of L1 and one of its analogues namely 2-methy-3-hydroxypyridin-4-one (L2), which possesses a higher partition coefficient (Kpart) than L...

Density functional theory (DFT) calculations have been carried out for a series of Cu(I) complexes bearing N-hexadentate macrocyclic dinucleating ligands and for their corresponding peroxo species (1c-8c) generated by their interaction with molecular O2. For complexes 1c-7c, it has been found that the side-on peroxodicopper(II) is the favored structure with regard to the bis(mu-oxo)dicopper(III...

Tripodal hexadentate hydroxypyridin-4-ones are increasingly utilised as iron(III) and gallium(III) ligands, their attachment to proteins being particularly useful for positron emission tomography (PET). A widely studied tripodal ligand NTA(BuHP)3, which is reported to form 1:1 iron(III) and gallium(III) complexes in aqueous, media forms 2:2 complexes under physiological conditions. This importa...

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...