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首页> 外文期刊>Journal of the Brazilian Chemical Society >Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity
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Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity

机译：3,5-二芳基异恶唑衍生物的合成及体外锥虫活性的评价

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Chagas disease is included in the neglected tropical diseases list and is endemic to 21 Latin American countries. The two drugs currently available for treating Chagas disease are nifurtimox and benznidazole and both result in many significant side effects. The study describes the synthesis and biological evaluation of 3,5-disubstituted isoxazoles. Isoxazoles were obtained by reaction of flavones and hydroxylamine and either alkylated at the free hydroxyl group and/or nitrated at the isoxazole ring. These compounds were evaluated for their in vitro anti-Trypanosoma cruzi activity against trypomastigote and amastigote forms of the parasite in T. cruzi-infected cell lineages. Benznidazole was used as a reference compound for the in vitro assay and mammalian L929 cells were employed to evaluate cytotoxicity. A majority of the compounds tested were very active and the most active isoxazole against amastigote and trypomastigotes of T. cruzi was slightly more potent than the current medicine benznidazole.
机译：恰加斯病被列入被忽视的热带病清单，并且是21个拉丁美洲国家的地方病。目前可用于治疗南美锥虫病的两种药物是尼富替莫和苯硝唑，它们均会导致许多明显的副作用。该研究描述了3,5-二取代异恶唑的合成和生物学评估。通过黄酮与羟胺反应得到异恶唑，并在游离羟基处烷基化和/或在异恶唑环上硝化。评估了这些化合物的体外抗锥虫锥虫和锥虫感染的细胞谱系中的锥虫和鞭毛体形式的寄生虫活性。苯并咪唑用作体外测定的参考化合物，哺乳动物L929细胞用于评估细胞毒性。测试的大多数化合物具有很高的活性，而对克氏锥虫的鞭毛象和锥鞭毛象的活性最强的异恶唑比目前的药物苯甲硝唑稍强。

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