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Orally active alpha-ketohydroxypyridine iron chelators: studies in mice

GJ Kontoghiorghes

Several N-substituted 3-hydroxypyrid-2-one and N-substituted 2-methyl-3- hydroxypyrid-4-one chelators were screened for 59Fe removal using iron- overloaded mice labeled with 59Fe. The most effectice chelators were found to be the N-methyl, N-ethyl, and N-propyl derivatives of 2-methyl- 3-hydroxypyrid-4-one. When the above three chelators were administered intragastrically or intraperitoneally (200 mg/kg) to mice, they caused equivalent 59Fe excretions to intraperitoneal desferrioxamine (200 mg/kg). These results increase the prospects for the use of the alpha- ketohydroxypyridine chelators in the treatment of iron overload.

Volume 30, Issue 6, pp. 670-673, 12/01/1986
Copyright © 1986 by American Society for Pharmacology and Experimental Therapeutics






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Copyright © 1986 by the American Society for Pharmacology and Experimental Therapeutics