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Start Over Author "Zidong Lu" Journal european journal of medicinal chemistry
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1. Systematic comparison of the mono-, dimethyl- and trimethyl 3-hydroxy-4(1H)-pyridones - Attempted optimization of the orally active iron chelator, deferiprone

Author

Zidong Lu, Robert C. Hider, Yuanyuan Xie, Sukhi Bansal, Xiaole Kong, and Tao Zhou

Subjects
Stereochemistry, Pyridones, Electrospray ionization, Administration, Oral, 010402 general chemistry, Iron Chelating Agents, 01 natural sciences, chemistry.chemical_compound, Drug Discovery, Humans, Deferiprone, Solid phase extraction, Acetonitrile, Pharmacology, chemistry.chemical_classification, 010405 organic chemistry, Dimethyl sulfoxide, Organic Chemistry, General Medicine, Hydrogen-Ion Concentration, 0104 chemical sciences, Orally active, Enzyme, chemistry, Microsomes, Liver
Abstract

A range of close analogues of deferiprone have been synthesised. The group includes mono-, di- and tri-methyl-3-hydroxy-4(1H)-pyridones. These compounds were found to possess similar pFe3+ values to that of deferiprone, with the exception of the 2.5-dimethylated derivatives. Surprisingly the NH-containing hydroxy-4(1H)-pyridones were found to be marginally more lipophilic than the corresponding N-Me containing analogues. This same group are also metabolised less efficiently by Phase 1 hydroxylating enzymes than the corresponding N-Me analogues. As result of this study, three compounds have been identified for further investigation centred on neutropenia and agranulocytosis.

Published
2015

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