Insight into the bioreductive mode of action of antitrypanosomal 5-nitrofuryl containing thiosemicarbazones.

Otero L; Maya JD; Morello A; Rigol C; Barriga G; Rodriguez J; Folch C; Norambuena E; Gonzalez M; Azar CO; Cerecetto H; Gambino D

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Insight into the bioreductive mode of action of antitrypanosomal 5-nitrofuryl containing thiosemicarbazones.

机译：深入了解抗锥虫5-硝基呋喃基硫代半脲的生物还原作用方式。

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In order to get insight into the trypanocidal mechanism of action of a series of 5-nitrofuryl containing thiosemicarbazones some studies related to their bioreduction were performed. Electron spin resonance spectra of radicals generated in T. cruzi by compounds' bioreduction were analyzed. Three different patterns of ESR signals were observed for the different assayed compounds. These results were in agreement with the changes in the T. cruzi-oxygen uptake promoted by these compounds. On the other hand, free-radical scavenger properties, measured as oxygen radical absorbance capacity (ORAC), did not seem to correlate with the trypanocidal activity.

机译：为了深入了解一系列含5-硝基呋喃基的硫半脲的锥虫作用机理，进行了一些与其生物还原有关的研究。分析了通过化合物的生物还原作用在克鲁维酵母中产生的自由基的电子自旋共振谱。对于不同的测定化合物，观察到了三种不同的ESR信号模式。这些结果与这些化合物所促进的克鲁维酵母吸收的变化是一致的。另一方面，以氧自由基吸收能力（ORAC）衡量的自由基清除剂性能似乎与锥虫杀虫活性无关。

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《Medicinal chemistry》 |2008年第1期|共7页
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Otero L; Maya JD; Morello A; Rigol C; Barriga G; Rodriguez J; Folch C; Norambuena E; Gonzalez M; Azar CO; Cerecetto H; Gambino D;
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中图分类药学;
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1. Insight into the bioreductive mode of action of antitrypanosomal 5-nitrofuryl containing thiosemicarbazones. [J] . Otero L, Maya JD, Morello A, Medicinal chemistry . 2008,第1期

机译：深入了解抗锥虫5-硝基呋喃基硫代半脲的生物还原作用方式。
2. In vitro activity and mechanism of action against the protozoan parasite Trypanosoma cruzi of 5-nitrofuryl containing thiosemicarbazones. [J] . Aguirre G, Boiani L, Cerecetto H, Bioorganic and medicinal chemistry . 2004,第18期

机译：含5-硝基呋喃硫半脲的原生动物寄生虫克氏锥虫的体外活性和作用机理。
3. In vitro activity and mechanism of action against the protozoan parasite Trypanosoma cruzi of 5-nitrofuryl containing thiosemicarbazones. [J] . Aguirre G, Boiani L, Cerecetto H, Bioorganic and Medicinal Chemistry . 2004,第18期

机译：含5-硝基呋喃硫半脲的原生动物寄生虫克氏锥虫的体外活性和作用机理。
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机译：一种在药理学中用于药物作用的结构活性方法：（A）DT-黄递酶（NQO1）介导的抗癌生物还原苯醌烷基化剂的还原动力学和作用方式的结构活性关系。（B）肾小管有机阳离子分泌所需的新型NMDA受体拮抗剂的结构特征。
6. Insights into antitrypanosomal drug mode-of-action from cytology-based profiling [O] . James A. Thomas, Nicola Baker, Sebastian Hutchinson, 2018

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Insight into the bioreductive mode of action of antitrypanosomal 5-nitrofuryl containing thiosemicarbazones.

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