PMID: 11902801Mar 21, 2002Paper

Synthesis and physicochemical assessment of novel 2-substituted 3-hydroxypyridin-4-ones, novel iron chelators

The Journal of Pharmacy and Pharmacology
Majid Y MoridaniR C Hider

Abstract

Novel 3-hydroxypyridin-4-one containing tridentate ligands were synthesised and their physicochemical properties characterised, including ionisation constants and stoichiometric titration with Fe(III). There is an urgent demand for orally active iron chelators with potential for the treatment of thalassaemia. In principle, tridentate ligands are likely to be more kinetically stable than bidentate molecules, but to date no satisfactory molecules have been identified. Fe(III) stability constants were assessed by competition with the hexadentate ligand EDTA. In all cases no evidence was found for a tridentate mode of iron chelation; instead the ligands behaved as bidentate hydroxypyridinones. As a consequence they provide no advantage over the more simple alkyl hydroxypyridinones.

References

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Citations

Jan 23, 2015·Chemical Communications : Chem Comm·Tao ZhouXiaole Kong
Mar 7, 2012·Dalton Transactions : an International Journal of Inorganic Chemistry·Tao ZhouRobert C Hider
May 8, 2010·Dalton Transactions : an International Journal of Inorganic Chemistry·Sofia GamaM Amélia Santos
Jul 24, 2018·Chemical Reviews·Agostino CilibrizziRobert C Hider

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