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首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >Evaluating anti-Toxoplasma gondii activity of new serie of phenylsemicarbazone and phenylthiosemicarbazones in vitro
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Evaluating anti-Toxoplasma gondii activity of new serie of phenylsemicarbazone and phenylthiosemicarbazones in vitro

机译：体外评估苯基半脲和苯硫代半脲的新系列抗弓形虫活性

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摘要

While Toxoplasma gondii is able to infect and replicate within all eukaryotic cells, tachyzoites are the infective form of T. gondii that invades all eukaryotic cells leading to tissue rupture, the main features of toxoplasmosis. The present study evaluates the activity of (benzaldehyde)-4-phenyl-3-thiosemicarbazone and (benzaldehyde)-(4 or 1)-phenylsemicarbazone against intracellular T. gondii. The nine new compounds were incubated in infected Vero cells at concentrations of 0.01, 0.1, 0.5, and 1.0 mM and evaluated for three main effects: cytotoxicity, infection, and number of intracellular parasites. The cytotoxicity test showed a pattern by analyzing the substituent arylhydraz-one, where trihydroxy Compounds 4-9 were cytotoxic at concentrations of 0.5 and 1.0 mM. The results highlight Compound 8, which reduced the number of intracellular parasites by 82 % in a concentration of 0.01 mM and showed a LD50 of 0.3 mM in cell culture. These different biological actions are due to changes in the molecular structure and type of radical present in each compound. All compounds tested were more efficient than the control drug sulfadizine.
机译：虽然弓形虫能够感染并在所有真核细胞中复制，但速殖子是弓形虫的感染形式，它侵袭了所有导致组织破裂的真核细胞，这是弓形虫病的主要特征。本研究评估了（苯甲醛）-4-苯基-3-硫代半脲和（苯甲醛）-（4或1）-苯基​​半脲对细胞内弓形虫的活性。将这九种新化合物以0.01、0.1、0.5和1.0 mM的浓度在感染的Vero细胞中孵育，并评估三种主要作用：细胞毒性，感染和细胞内寄生虫的数量。细胞毒性试验通过分析取代基芳基肼一显示出一种模式，其中三羟基化合物4-9在浓度为0.5和1.0 mM时具有细胞毒性。结果突出显示了化合物8，该化合物在0.01 mM的浓度下可将细胞内寄生虫的数量减少82％，并在细胞培养中显示LD50为0.3 mM。这些不同的生物学作用是由于每种化合物中存在的分子结构和自由基类型的变化。测试的所有化合物均比对照药物磺胺嘧啶更有效。

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