喹啉-4(1H)-亚胺是针对疟疾肝期的强效抗疟药物。
Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria.
机构信息
Research Institute for Medicines and Pharmaceutical Sciences (iMed.UL), Faculty of Pharmacy, University of Lisbon, Avenida Prof. Gama Pinto, 1649-019 Lisbon, Portugal.
出版信息
J Med Chem. 2013 Jun 13;56(11):4811-5. doi: 10.1021/jm400246e. Epub 2013 May 23.
We present a novel series of quinolin-4(1H)-imines as dual-stage antiplasmodials, several-fold more active than primaquine in vitro against Plasmodium berghei liver stage. Among those, compounds 5g and 5k presented low nanomolar IC50 values. The compounds are metabolically stable and modulate several drug targets. These results emphasize the value of quinolin-4(1H)-imines as a new chemotype and their suitable properties for further drug development.
我们提出了一系列新型的喹啉-4(1H)-亚胺作为双阶段抗疟原虫药物，对伯氏疟原虫肝期的体外活性比普喹酮高几倍。其中，化合物 5g 和 5k 的 IC50 值低至纳摩尔级。这些化合物具有代谢稳定性，并调节多种药物靶点。这些结果强调了喹啉-4(1H)-亚胺作为一种新型化学型的价值，以及它们适合进一步药物开发的特性。
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