Partition coefficients of the iron(III) complexes of pyridoxal isonicotinoyl hydrazone and its analogs and the correlation to iron chelation efficacy

✍ Scribed by J. T. Edward; P. Ponka; D. R. Richardson

• Publisher: Springer Netherlands
• Year: 1995
• Tongue: English
• Weight: 558 KB
• Volume: 8
• Category: Article
• ISSN: 1572-8773
• DOI: 10.1007/bf00143378

✦ Synopsis

Pyridoxal isonicotinoyl hydrazone and its analogs are orally effective Fe(llI) chelators which show potential as drugs to treat iron overload disease. The present investigation describes the measurement of the partition coefficient of the apochclator and Fe(lll) complex of 20 of these ligands. These measurements have been done to investigate the relationship between lipophilicity and the efficacy of iron chelation in rabbit reticulocytes loaded with non-heme S9Fe. The results demonstrate a linear relationship between the partition coefficient (P) of the apochelator and its Fe(lll) complex, and a simple equation has been derived relating these two parameters. Experimental data in the literature are in agreement with the equation. The relationship of the partition coefficients of the iron chelators and of their Fe(lll) complexes to the effectiveness of the ligands in mobilizing iron in vitro and in vivo is also discussed.