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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and antimalarial activity of semicarbazone and thiosemicarbazone derivatives.
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Synthesis and antimalarial activity of semicarbazone and thiosemicarbazone derivatives.

机译：半卡巴zone和硫代半卡巴zone衍生物的合成及其抗疟活性。

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摘要

Seventeen semicarbazone and thiosemicarbazone derivatives were prepared and tested in vitro against a chloroquine resistant strain of Plasmodium falciparum (W2) to evaluate their antiplasmodial potential. Three thiosemicarbazones were found to be active against the parasite and non-toxic to human peripheral blood mononuclear cells (PBMC). Among these, compound 5b presented the lowest IC50 value against P. falciparum (7.2 microM) and was the least toxic in the PBMC proliferation assay (IC50=73.5 microM). It was selected for in vivo tests on mice infected with Plasmodium berghei (strain NK-65). The thiosemicarbazone 5b was able to reduce the parasitaemia by 61% at 20 mg/kg on day 7 after infection without any sign of toxicity to the animals. In comparison, the standard drug chloroquine at 15 mg/kg showed a reduction around 95%. These in vitro and in vivo results make 5b an interesting lead for further development.
机译：制备了十七种半卡巴zone和硫代半卡巴zone衍生物，并在体外针对恶性疟原虫（W2）的耐氯喹菌株进行了测试，以评估其抗血浆的潜力。发现三种硫代半脲酮对寄生虫具有活性，并且对人外周血单核细胞（PBMC）无毒。其中，化合物5b对恶性疟原虫的IC50值最低（7.2 microM），在PBMC增殖试验中毒性最低（IC50 = 73.5 microM）。选择它用于感染伯氏疟原虫（NK-65株）的小鼠体内测试。感染后第7天，硫半脲5b能够以20 mg / kg的剂量将寄生虫血症降低61％，而对动物没有任何毒性迹象。相比之下，标准药物氯喹（15毫克/千克）显示减少约95％。这些体外和体内结果使5b成为进一步开发的有趣线索。

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