首页> 美国卫生研究院文献>Malaria Journal >In vitro antiplasmodial activity pharmacokinetic profiles and interference in isoprenoid pathway of 2-aniline-3-hydroxy-1.4-naphthoquinone derivatives
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In vitro antiplasmodial activity pharmacokinetic profiles and interference in isoprenoid pathway of 2-aniline-3-hydroxy-1.4-naphthoquinone derivatives

机译:2-苯胺-3-羟基-1.4-萘醌衍生物的体外抗血浆活性药动学特征和对类异戊二烯途径的干扰

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摘要

BackgroundPlasmodium falciparum has shown multidrug resistance, leading to the necessity for the development of new drugs with novel targets, such as the synthesis of isoprenic precursors, which are excellent targets because the pathway is different in several steps when compared with the human host. Naphthoquinone derivatives have been described as potentially promising for the development of anti-malarial leader molecules. In view of that, the focus in this work is twofold: first, evaluate the in vitro naphthoquinone antiplasmodial activity and cytotoxicity; secondly, investigate one possible action mechanism of two derivatives of hydroxy-naphthoquinones.
机译:背景恶性疟原虫已显示出多药耐药性,因此有必要开发具有新型靶标的新药,例如合成异戊二烯前体,它们是极好的靶标,因为与人类宿主相比,该途径在几个步骤上有所不同。萘醌衍生物被描述为开发抗疟疾前导分子的潜在前途。有鉴于此,这项工作的重点是双重的:首先,评估体外萘醌的抗血浆活性和细胞毒性。其次,研究了两种羟基萘醌衍生物的可能作用机理。

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