Figure 1.

The design of the alpha-ketohydroxypyridine and alpha-ketohydroxypyrone iron chelators for clinical use. The chemical structures of four classes of iron chelators, namely 3-hydroxypyrid-4-ones (I), 3-hydroxypyrid-2-ones (II), 1-hydroxypyrid-2-ones (III) and 3-hydroxypyr-4-ones (IV), were identified 40 years ago, following a structure–activity simulation based on the prototype structures of the known compounds mimosine (V), tropolone (VI), 1-hydroxypyrid-2-one (VII) and maltol (VIII). Chemical synthesis and iron binding studies led to the development of the drugs deferiprone (L1) and maltol–iron for the treatment of iron overload and iron deficiency anemia, respectively (see [60]).