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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Deferitazole, a new orally active iron chelator
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Deferitazole, a new orally active iron chelator

机译：Deferitazole，一种新型口服活性铁螯合剂

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摘要

Following a systematic search of desferrithiocin analogs, a polyether derivative, deferitazole (formerly FBS0701), has entered into phase 1 and 2 clinical trials with promising biological properties. However, until now, detailed physicochemical properties of this chelator have not been reported. The compound displays a high affinity and selectivity for iron(III) as demonstrated by the log beta(2) = 33.39 +/- 0.03 and the pFe(3+) value of 22.3. Two equilibrating isomeric forms of the iron(III) complex exist under biological conditions. Deferitazole also binds the trivalent metals Al-III and La-III with high affinity; log beta(2) values, 26.68 and 21.55 respectively. The affinity of deferitazole for divalent cations is somewhat lower, with the exception of Cu-II which possesses a log beta(2) value of 25.5; deferitazole scavenges iron from labile sources such as citrate and albumin with efficiencies comparable with those of other therapeutic iron chelators, including deferasirox, deferiprone and desferrioxamine. The Fe-III(deferitazole)(2) is stable under physiological conditions and does not redox cycle. The high affinity of deferitazole for iron(III) renders it unlikely that this chelator will lead to the redistribution of iron and consequently deferitazole shows considerable promise as a therapeutic iron(III) chelator.
机译：在对去铁硫代类似物进行系统搜索之后，聚醚衍生物去铁唑（以前的FBS0701）已经进入具有良好生物学特性的1期和2期临床试验。但是，到目前为止，尚未报道该螯合剂的详细理化性质。该化合物显示出对铁（III）的高亲和力和选择性，如log beta（2）= 33.39 +/- 0.03和pFe（3+）值22.3所示。铁（III）配合物的两种平衡异构形式在生物学条件下存在。 Deferitazole还以高亲和力结合三价金属Al-III和La-III。记录beta（2）值，分别为26.68和21.55。去铁唑对二价阳离子的亲和力稍低，但Cu-II的log beta（2）值为25.5。去铁唑从不稳定的来源（如柠檬酸盐和白蛋白）中清除铁，其效率可与其他治疗性铁螯合剂（包括地拉罗司，去铁酮和去铁胺）相媲美。 Fe-III（deferitazole）（2）在生理条件下稳定，并且没有氧化还原循环。去铁唑对铁（III）的高亲和力使得该螯合剂不太可能导致铁的重新分布，因此去铁唑显示出作为治疗性铁（III）螯合剂的巨大希望。

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