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Quinine conjugates and quinine analogues as potential antimalarial agents

机译:奎宁偶联物和奎宁类似物作为潜在的抗疟药

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摘要

Malaria is a tropical disease, prevalent in Southeast Asia and Africa, resulting in over half a million deaths annually; efforts to develop new antimalarial agents are therefore particularly important. Quinine continues to play a role in the fight against malaria, but quinoline derivatives are more widely used. Drugs based on the quinoline scaffold include chloroquine and primaquine, which are able to act against the blood and liver stages of the parasite's life cycle. The purpose of this review is to discuss reported biologically active compounds based on either the quinine or quinoline scaffold that may have enhanced antimalarial activity. The review emphasises hybrid molecules, and covers advances made in the last five years. The review is divided into three sections: modifications to the quinine scaffold, modifications to aminoquinolines and finally metal-containing antimalarial compounds. (C) 2015 Elsevier Masson SAS. All rights reserved.
机译:疟疾是一种热带疾病,流行于东南亚和非洲,每年导致超过半百万人死亡。因此,开发新的抗疟药的努力尤其重要。奎宁继续在抗击疟疾中发挥作用,但喹啉衍生物得到更广泛的应用。基于喹啉骨架的药物包括氯喹和伯氨喹,它们能够对抗寄生虫生命周期的血液和肝脏阶段。这篇综述的目的是讨论基于奎宁或喹啉骨架的报道的具有增强抗疟活性的生物活性化合物。这篇综述强调了杂化分子,并涵盖了过去五年中取得的进展。该综述分为三个部分:对奎宁支架的修饰,对氨基喹啉的修饰以及最后是含金属的抗疟化合物。 (C)2015 Elsevier Masson SAS。版权所有。

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