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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents.
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Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents.

机译:杂合4-氨基喹啉三嗪作为一类新型抗疟药的合成和生物评价。

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摘要

The emergence and rapid spread of chloroquine resistant strains of Plasmodium falciparum has dramatically reduced the chemotherapeutic options. Towards this goal, a series of new class of hybrid 4-aminoquinoline triazines were synthesized and screened against CQ sensitive strain 3D7 of P. falciparum in an in vitro model. Compounds 65 and 69 exhibited more than 99% suppression on day 4 and on day 6 post treatment, compound 69 showed impressive 99.11% suppression against CQ resistant strain N-67 of P. yoelii in an in vivo assay.
机译:恶性疟原虫的氯喹抗药性菌株的出现和迅速传播极大地减少了化学疗法的选择。为了实现这一目标,合成了一系列新型的杂种4-氨基喹啉三嗪,并在体外模型中针对恶性疟原虫的CQ敏感菌株3D7进行了筛选。在体内试验中,化合物65和69在治疗后的第4天和第6天表现出超过99%的抑制,化合物69显示出对约氏疟原虫的CQ抗性菌株N-67的令人印象深刻的99.11%抑制。

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