Relative oral efficacy and acute toxicity of hydroxypyridin-4-one iron chelators in mice [see comments]

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Relative Oral Efficacy and Acute Toxicity of Hydroxypyridin-4-One Iron Chelators in Mice

The relationship between the oral efficacy and the acute toxicity of hydroxypyridin4one iron chelators has been investigated to clarify structure-function relationships of these compounds in vivo and to identify compounds with the maximum therapeutic safety margin. By comparing “Fe excretion following oral or intraperitoneal administration of increasing doses of each chelator to iron-overloaded...

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Relative oral efficacy and acute toxicity of hydroxypyridin-4-one iron chelators in mice.

The relationship between the oral efficacy and the acute toxicity of hydroxypyridin-4-one iron chelators has been investigated to clarify structure-function relationships of these compounds in vivo and to identify compounds with the maximum therapeutic safety margin. By comparing 59Fe excretion following oral or intraperitoneal administration of increasing doses of each chelator to iron-overloa...

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Comparison of the subacute toxicity and efficacy of 3-hydroxypyridin-4-one iron chelators in overloaded and nonoverloaded mice.

Five orally effective iron chelators of the 3-hydroxypyridin-4-one series have been administered intraperitoneally to iron-overloaded and nonoverloaded male mice at a dose of 200 mg/kg/24 h for a total of 60 days to investigate the effect on iron loading and toxicity. There was a significant reduction in hepatic iron at the end of the study in the iron-overloaded mice with all compounds studied...

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Evaluation of Liver Toxicity of 2-Methyl-3-Hydroxypyridin-4-one in Iron Overloaded Rats

      Hydroxypyridinone iron chelators are currently the main candidates for development of orally active iron chelating alternatives to desferrioxamine (DFO). In the present study, the relative efficacy and liver toxicity of a bidentate chelator, 2-methyl-3-hydroxypyridin-4-one (MHPO), was studied in iron overloaded rats and compared with those of DFO. For iron overloading, rats received i.p. ...

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The effect of N-alkyl modification on the antimalarial activity of 3-hydroxypyridin-4-one oral iron chelators.

The antimalaria effect of iron chelators is attributed to their interaction with a labile iron pool within parasitised erythrocytes, and it was postulated that increased affinity to iron as well as increased lipophilicity may improve antimalarial activity. In the present study we have examined the antimalarial effect of 3-hydroxypyridin-4-ones, a family of bidentate orally effective iron chelat...

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ژورنال

عنوان ژورنال: Blood

سال: 1990

ISSN: 0006-4971,1528-0020

DOI: 10.1182/blood.v76.11.2389.2389