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2,4-二芳基噻唑类抗朊病毒化合物作为一类新型抗疟先导化合物。

2,4-diarylthiazole antiprion compounds as a novel structural class of antimalarial leads.

机构信息

Department of Chemistry, University of Sheffield, Brook Hill, Sheffield, UK.

出版信息

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3644-7. doi: 10.1016/j.bmcl.2011.04.090. Epub 2011 Apr 28.

Abstract

A significant intersection between antimalarial and antiprion activity is well established for certain compound classes, specifically for polycyclic antimalarial agents bearing basic nitrogen-containing sidechains (e.g., chloroquine, quinacrine, mefloquine). Screening a recently reported set of antiprion compounds with such sidechains showed these 2,4-diarylthiazole based structures also possess significant antimalarial activity. Of particular note, all but one of the compounds displayed activity against a chloroquine-resistant Plasmodium falciparum strain, identifying them as interesting leads for further development in this context. In addition, three new members of the series showed superior antiprion activity compared to the earlier-reported compounds.

摘要

某些化合物类别(例如,含碱性氮侧链的多环抗疟药物[如氯喹、奎宁、甲氟喹])的抗疟和抗朊病毒活性之间存在显著的交叉。用具有此类侧链的最近报道的一组抗朊病毒化合物进行筛选表明,这些基于 2,4-二芳基噻唑的结构也具有显著的抗疟活性。值得特别注意的是,除了一种化合物外,所有化合物对氯喹耐药的恶性疟原虫株均有活性,这表明它们是这方面进一步开发的有趣先导化合物。此外,该系列的三个新成员与之前报道的化合物相比,表现出更好的抗朊病毒活性。

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