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新型疟原虫电子传递链抑制剂。

Novel inhibitors of the Plasmodium falciparum electron transport chain.

机构信息

Liverpool School of Tropical Medicine, Pembroke Place, Liverpool, L3 5QA, UK.

Department of Chemistry, University of Liverpool, P.O. Box 147, Liverpool, L69 3BX, UK.

出版信息

Parasitology. 2014 Jan;141(1):50-65. doi: 10.1017/S0031182013001571.

Abstract

Due to an increased need for new antimalarial chemotherapies that show potency against Plasmodium falciparum, researchers are targeting new processes within the parasite in an effort to circumvent or delay the onset of drug resistance. One such promising area for antimalarial drug development has been the parasite mitochondrial electron transport chain (ETC). Efforts have been focused on targeting key processes along the parasite ETC specifically the dihydroorotate dehydrogenase (DHOD) enzyme, the cytochrome bc 1 enzyme and the NADH type II oxidoreductase (PfNDH2) pathway. This review summarizes the most recent efforts in antimalarial drug development reported in the literature and describes the evolution of these compounds.

摘要

由于对抗疟原虫具有强大疗效的新型抗疟化学疗法的需求不断增加,研究人员正在针对寄生虫内的新过程进行研究,以避免或延迟耐药性的出现。寄生虫线粒体电子传递链 (ETC) 是抗疟药物开发的一个很有前途的领域。研究工作集中在针对寄生虫 ETC 的关键过程上,特别是二氢乳清酸脱氢酶 (DHOD) 酶、细胞色素 bc1 酶和 NADH 型 II 氧化还原酶 (PfNDH2) 途径。本综述总结了文献中报道的最新抗疟药物开发工作,并描述了这些化合物的演变过程。

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