Design, synthesis and evaluation of N-basic substituted 3-hydroxypyridin-4-ones: orally active iron chelators with lysosomotrophic potential

…, HH KHODR, SL Lu, RC HIDER

Index: Liu, Zu D.; Khodr, Hicham H.; Lu, Shu L.; Hider, Robert C. Journal of Pharmacy and Pharmacology, 2000 , vol. 52, # 3 p. 263 - 272

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Citation Number: 15

Abstract

Abstract To investigate the possibility of targeting chelators into the lysosomal iron pool, nine bidentate 3-hydroxypyridin-4-ones with basic chains have been synthesized. As the turnover of ferritin iron is centred in the lysosome, such strategy is predicted to increase chelator efficacy of bidentate ligands. The pKa values of the ligands together with their distribution coefficients between 1- octanol and 4-morpholinepropane sulphonic acid (MOPS) buffer pH7Á4 have ...

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