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首页> 外文期刊>Journal of Medicinal Chemistry >N-Cinnamoylated chloroquine analogues as dual-stage antimalarial leads
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N-Cinnamoylated chloroquine analogues as dual-stage antimalarial leads

机译：N-肉桂酰氯喹类似物作为双阶段抗疟药物

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The control of malaria is challenged by drug resistance, and new antimalarial drugs are needed. New drug discovery efforts include consideration of hybrid compounds as potential multitarget antimalarials. Previous work from our group has demonstrated that hybrid structures resulting from cinnamic acid conjugation with heterocyclic moieties from well-known antimalarials present improved antimalarial activity. Now, we report the synthesis and SAR analysis of an expanded series of cinnamic acid derivatives displaying remarkably high activities against both blood-and liver-stage malaria parasites. Two compounds judged most promising, based on their in vitro activity and druglikeness according to the Lipinski rules and Veber filter, were active in vivo against blood-stage rodent malaria parasites. Therefore, the compounds reported represent a new entry as promising dual-stage antimalarial leads.
机译：耐药性挑战了疟疾的控制，因此需要新的抗疟药。新药开发工作包括将杂合化合物视为潜在的多靶点抗疟药。我们小组以前的工作表明，肉桂酸与众所周知的抗疟疾药物的杂环部分结合产生的杂化结构具有改善的抗疟疾活性。现在，我们报告了一系列肉桂酸衍生物的合成和SAR分析，这些衍生物显示出对血液和肝脏阶段疟疾寄生虫均具有显着高活性。根据Lipinski规则和Veber过滤器，根据其体外活性和药物相似性，被认为最有前途的两种化合物在体内对血阶段啮齿类疟疾寄生虫具有活性。因此，所报道的化合物代表了有前途的双阶段抗疟药物。

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