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Synthesis of 4-aminoquinoline - Pyrimidine hybrids as potent antimalarials and their mode of action studies

机译:4-氨基喹啉-嘧啶杂化物的合成作为有效的抗疟药及其作用方式研究

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摘要

One of the most viable options to tackle the growing resistance to the antimalarial drugs such as artemisinin is to resort to synthetic drugs. The multi-target strategy involving the use of hybrid drugs has shown promise. In line with this, new hybrids of quinoline with pyrimidine have been synthesized and evaluated for their antiplasmodial activity against both CQS and CQR strains of Plasmodium falciparum. These depicted activity in nanomolar range and were found to bind to heme as well as AT rich pUC18 DNA.
机译:解决对青蒿素等抗疟药日益增长的耐药性的最可行选择之一是求助于合成药物。涉及使用杂种药物的多目标策略已显示出希望。为此,已经合成了喹啉和嘧啶的新杂种,并评估了它们对恶性疟原虫CQS和CQR菌株的抗疟原虫活性。这些描绘的活性在纳摩尔范围内,并发现与血红素以及富含AT的pUC18 DNA结合。

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