Recent updates in the development of mettallocenes with antimalarial activity

Jelena Aksic, Marija Gencic, N. Radulović
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引用次数: 2

Abstract

Great progress in the fight against malaria has been made in the last decade. Nevertheless, the development of resistance to almost all commonly used antimalarial drugs poses a major threat to the sustainability of this progress and highlights the need for the discovery of novel potent and inexpensive antimalarials to stay one step ahead. After the finding of ferrocene-containing analog of chloroquine - ferroquine, that can overcome Plasmodium resistance, a ?big-bang? in the metallocene antimalarials research has occurred. This review describes in detail the most recent advances in this important field of medicinal chemistry. Even though it is quite hard to beat ferroquine, it seems that this could be succeeded by suitable modifications in the structure of ferroquine, by the introduction of ? second metal center or through joining metallocenes with two or more proven antimalarial motifs into a single molecule.
具有抗疟活性的茂金属化合物的最新进展
过去十年在防治疟疾方面取得了巨大进展。然而,对几乎所有常用抗疟药物的耐药性的发展对这一进展的可持续性构成重大威胁,并突出表明需要发现新的有效和廉价的抗疟药物,以保持领先一步。在发现含二茂铁的氯喹类似物-亚铁喹后,发现可以克服疟原虫耐药性,这是一个“大爆炸”。在茂金属抗疟药方面已经开展了研究。本文详细介绍了这一重要药物化学领域的最新进展。尽管很难打败亚铁,但似乎可以通过对亚铁的结构进行适当的修饰,通过引入?第二个金属中心或通过将金属茂烯与两个或两个以上已证实的抗疟疾基序连接成一个单一分子。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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