Design, synthesis, and evaluation of novel 2-substituted 3-hydroxypyridin-4-ones: Structure-activity investigation of metalloenzyme inhibition by iron chelators
A range of novel 3-hydroxypyridin-4-ones with different R2 substitutents has been synthesized for the investigation of the structure-activity relationship between the chemical nature of the ligand and the inhibitory activity of the iron-contain
Liu, Zu D.,Kayyali, Reem,Hider, Robert C.,Porter, John B.,Theobald, Anthony E.
p. 631 - 639
(2007/10/03)
Synthesis, physicochemical properties, and biological evaluation of N- substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: Orally active iron chelators with clinical potential
The synthesis of a range of novel bidentate ligands containing the chelating moiety 3-hydroxy-4(1H)-pyridinone is described. The pK(a) values of the ligands and the stability constants of their iron(III) complexes have been determined. The crystal structures of one of the ligands and one of the iron(III) complexes are presented. The distribution coefficients of the ligands are reported and are related to the ability of the ligands to remove iron from hepatocytes. The influence of 3-hydroxy-4(1H)-pyridinones on oxidative damage to cells is described. In contrast to the iron chelator in current therapeutic use, desferrioxamine-B, many of the bidentate ligands described in this study are orally active in iron-overloaded mice.
Dobbin,Hider,Hall,Taylor,Sarpong,Porter,Xiao,Van der Helm
p. 2448 - 2458
(2007/10/02)
Crystal Structure of 3-Hydroxy-2-ethyl-1-methyl-, 3-Hydroxy-1,2-diethyl-, and 3-Hydroxy-2-ethyl-1-hexyl-pyridin-4(1H)-ones.
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Burgess, John,Fawcett, John,Patel, Marttand S.,Russell, David R.
p. 214 - 246
(2007/10/02)
Esterified hydroxy dihydropyridinones for treating diseases associated with trivalent metal ion overload
3-Substituted 4(1H)-pyridone compounds of formula STR1 wherein R1 is an unsubstituted or substituted hydrocarbon radical, X is a bond or a group of formula --O-- or --N(R3)--, wherein R3 is hydrogen or an unsubstituted or
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(2008/06/13)
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