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Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry

机译:一系列新型适用于流行化学的抗疟疾药物的鉴定和体外ADME评估

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摘要

Triage of a set of antimalaria hit compounds, identified through high throughput screening against the Chloroquine sensitive (3D7) and resistant (Dd2) parasite Plasmodium falciparum strains identified several novel chemotypes suitable for hit-to-lead chemistry investigation. The set was further refined through investigation of their in vitro ADME properties, which identified templates with good potential to be developed further as antimalarial agents. One example was profiled in an in vivo murine Plasmodium berghei model of malaria infection.
机译:通过对氯喹敏感(3D7)和耐药性(Dd2)寄生虫恶性疟原虫菌株进行高通量筛选,鉴定了一组抗疟疾重击化合物,鉴定出几种适用于从头到尾化学研究的新型化学型。通过研究其体外ADME特性进一步完善了该组合,确定了具有良好潜力的模板,可以进一步开发作为抗疟药。在疟疾感染的体内鼠伯氏疟原虫模型中描述了一个实例。

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