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首页> 外文期刊>Antimicrobial agents and chemotherapy. >Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes.
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Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes.

机译：三氧杂喹是新的抗疟疾剂，对所有红血球形式均有效，包括配子体细胞。

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摘要

Malaria is the third most significant cause of infectious disease in the world. The search for new antimalarial chemotherapy has become increasingly urgent due to parasite resistance to classical drugs. Trioxaquines are synthetic hybrid molecules containing a trioxane motif (which is responsible for the antimalarial activity of artemisinin) linked to an aminoquinoline entity (which is responsible for the antiplasmodial properties of chloroquine). These trioxaquines are highly potent against young erythrocytic stages of Plasmodium falciparum and exhibit efficient activity in vitro against chloroquine-sensitive and -resistant strains of P. falciparum (50% inhibitory concentration, 4 to 32 nM) and are also active in vivo against P. vinckei petteri and P. yoelii nigeriensis in suppressive and curative murine tests. The trioxaquine DU1302 is one of these promising antimalarial agents. The present study confirms the absence of toxicity of this drug on cell lines and in a mice model. Moreover, DU1302 exhibitspotent activity against gametocytes, the form transmitted by mosquitoes, as killing of the gametocytes is essential to limit the spread of malaria. The ease of chemical synthesis of this trioxaquine prototype should be considered an additional advantage and would make these drugs affordable without perturbations of the drug supply.
机译：疟疾是世界上第三大最重要的传染病原因。由于对经典药物的寄生虫耐药性，寻求新的抗疟疾化学疗法变得越来越紧迫。三恶喹是含有三恶烷基序（负责青蒿素的抗疟活性）和氨基喹啉实体（负责氯喹的抗血浆特性）的合成杂合分子。这些三氧喹喹对恶性疟原虫的年轻促红细胞生成期非常有效，并且在体外对氯喹敏感和耐药的恶性疟原虫菌株表现出有效的活性（50％抑制浓度，4至32 nM），并且在体内还对恶性疟原虫具有活性。 Vinckei petteri和P. yoelii nigeriensis在抑制性和治愈性小鼠测试中的作用。三恶喹DU1302是这些有前途的抗疟药之一。本研究证实了这种药物对细胞系和小鼠模型没有毒性。此外，DU1302对配子细胞表现出强大的活性，配子细胞是蚊子传播的形式，因为杀死配子细胞对于限制疟疾的传播至关重要。这种三氧喹喹原型的化学合成简便性应被认为是一个额外的优势，它将使这些药物价格可承受而不会干扰药物供应。

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