Synthesis, physicochemical characterization, and biological evaluation of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones: Novel iron chelators with enhanced pFe3+ …

…, HH Khodr, DY Liu, SL Lu, RC Hider

文献索引：Liu, Zu D.; Khodr, Hicham H.; Liu, Ding Y.; Lu, Shu L.; Hider, Robert C. Journal of Medicinal Chemistry, 1999 , vol. 42, # 23 p. 4814 - 4823

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被引用次数: 86

摘要

The synthesis of a range of 2-(1'-hydroxyalkyl)-3-hydroxypyridin-4-ones as bidentate iron (III) chelators with potential for oral administration is described. The p K a values of the ligands and the stability constants of their iron (III) complexes have been determined. Results indicate that the introduction of a 1'-hydroxyalkyl group at the 2-position leads to a significant improvement in the pFe3+ values. Such an effect was found to be greater with the ...