Ferroquine and its derivatives: new generation of antimalarial agents.
Ferroquine and its derivatives: new generation of antimalarial agents.
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DOI：
10.1016/j.ejmech.2015.07.009
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发表时间：
2015-08-28
影响因子：
6.7
通讯作者：
Hun LT
中科院分区：
文献类型：
--
作者：
Wani WA;Jameel E;Baig U;Mumtazuddin S;Hun LT
长期以来，疟疾一直困扰着人类。目前，市场上有几类抗疟药物，但毒性、疗效较低和疟原虫耐药性等问题降低了它们的总体治疗指数。因此，寻找新的有希望的抗疟疾药物的工作仍在继续，然而，与疟疾的斗争远未结束。Ferroquine是氯喹的衍生物，具有抗疟疾特性。它是最成功的氯喹衍生物。不仅铁喹，而且其衍生物已显示出作为临床感兴趣的抗疟药的有希望的潜力。目前，许多研究致力于开发铁喹衍生物作为抗疟化疗的安全替代品。本文介绍了铁喹的结构、化学和生物学特性。几类二茂铁衍生物，包括羟基二茂铁喹，三氧杂菲咯喹，氯喹桥连二茂铁，缩氨基硫脲衍生物，二茂铁双共轭物，4-N-取代衍生物，和其他已被讨论。此外，还对铁喹的作用机理进行了探讨。本文对一些疗效优于或等同于氯喹和铁喹的具有重要意义的铁喹衍生物进行了仔细的观察。本文对铁喹衍生物的毒性作了简要的讨论。最后，讨论了基于铁喹的抗疟药物开发的当前挑战和未来前景。讨论了铁喹的结构、化学和生物学特性。综述了几类二茂铁喹衍生物。已描述了Ferroquine的作用机制。着重指出了以铁喹为基础的抗疟药物开发方面的挑战。概述了基于铁奎宁的抗疟药物开发的前景。
Malaria has been teasing human populations from a long time. Presently, several classes of antimalarial drugs are available in market, but the issues of toxicity, lower efficacy and the resistance by malarial parasites have decreased their overall therapeutic indices. Thus, the search for new promising antimalarials continues, however, the battle against malaria is far from over. Ferroquine is a derivative of chloroquine with antimalarial properties. It is the most successful of the chloroquine derivatives. Not only ferroquine, but also its derivatives have shown promising potential as antimalarials of clinical interest. Presently, much research is dedicated to the development of ferroquine derivatives as safe alternatives to antimalarial chemotherapy. The present article describes the structural, chemical and biological features of ferroquine. Several classes of ferroquine derivatives including hydroxyferroquines, trioxaferroquines, chloroquine-bridged ferrocenophanes, thiosemicarbazone derivatives, ferrocene dual conjugates, 4-N-substituted derivatives, and others have been discussed. Besides, the mechanism of action of ferroquine has been discussed. A careful observation has been made into pharmacologically significant ferroquine derivatives with better or equal therapeutic effects to that of chloroquine and ferroquine. A brief discussion of the toxicities of ferroquine derivatives has been made. Finally, efforts have been made to discuss the current challenges and future perspectives of ferroquine-based antimalarial drug development. Structural, chemical and biological features of ferroquine have been discussed. Several classes of ferroquine derivatives have been reviewed. Mechanism of action of ferroquine has been described. Challenges in ferroquine-based antimalarial drug development have been highlighted. Perspectives in ferroquine-based antimalarial drug development have been outlined.
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