5-Nitro-2-furyl derivative actives against Trypanosoma cruzi: preliminary in vivo studies.

Cabrera E; Murguiondo MG; Arias MG

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5-Nitro-2-furyl derivative actives against Trypanosoma cruzi: preliminary in vivo studies.

机译：5-硝基-2-呋喃基衍生物对克鲁斯锥虫的活性：体内初步研究。

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Ten 5-nitro-2-furyl derivatives, with good to excellent in vitro anti-Trypanosoma cruzi activity, and nifurtimox were tested oral and intraperitoneally on healthy animals for its acute toxicity on murine models. According to animals' survival percentage, organ histological results, biochemical and haematological findings, three new derivatives, with toxicity like nifurtimox, were selected to test in vivo as antichagasic agents. Clearly, dependences between chemical structure and both acute toxicity and in vivo anti-T. cruzi activity were observed. 4-Hexyl-1-[3-(5-nitro-2-furyl)-2-propenylidene]semicarbazide displayed good profile as anti-T. cruzi agent and better acute toxicity profile than nifurtimox.

机译：在健康动物中口服和腹膜内测试了十种具有良好或优异的体外抗克氏锥虫活性的5-硝基-2-呋喃基衍生物和硝呋替莫，以证明它们对鼠模型具有急性毒性。根据动物的存活率，器官组织学结果，生化和血液学发现，选择了三种具有毒性的新衍生物，如硝呋替莫斯（nifurtimox），作为抗chachagasic剂进行体内测试。显然，化学结构与急性毒性和体内抗T之间存在依赖性。观察到了克鲁兹活性。 4-己基-1- [3-（5-硝基-2-呋喃基）-2-丙烯基]氨基脲显示出良好的抗T特性。与尼呋替莫相比，它具有克鲁索剂和更好的急性毒性。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2009年第10期|共6页
作者
Cabrera E; Murguiondo MG; Arias MG;
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正文语种 eng
中图分类医药、卫生;劳动卫生;
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1. 5-Nitro-2-furyl derivative actives against Trypanosoma cruzi: preliminary in vivo studies. [J] . Cabrera E, Murguiondo MG, Arias MG European Journal of Medicinal Chemistry: Chimie Therapeutique . 2009,第10期

机译：5-硝基-2-呋喃基衍生物对克鲁斯锥虫的活性：体内初步研究。
2. Antiproliferative effects and mechanism of action of SCH 56592 against Trypanosoma (Schizotrypanum) cruzi: in vitro and in vivo studies. [J] . Urbina JA, Payares G, Contreras LM, Antimicrobial agents and chemotherapy. . 1998,第7期

机译：SCH 56592对克氏锥虫的抗增殖作用及其作用机理：体内和体外研究。
3. New potent 5-nitroindazole derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and mechanism of action studies. [J] . Rodriguez J, Aran VJ, Boiani Bioorganic and medicinal chemistry . 2009,第24期

机译：新型有效的5-硝基吲唑衍生物作为克氏锥虫生长的抑制剂：合成，生物学评估和作用机理研究。
4. Study of optically trapped living Trypanosoma cruzi/Trypanosoma rangeli - Rhodnius prolixus interactions by real time confocal images using CdSe quantum dots [C] . A. A. de Thomaz, D. B. Almeida, W. M. Faustino, Conference on optical trapping and optical micromanipulation . 2008

机译：光学捕获的活锥虫瘤rangeli / rangli - rangnius rangeli - rangnius rangeli使用Cdse量子点的实时共焦图像相互作用
5. Design, synthesis, and biological evaluation of molecules of medicinal interest: Inhibitors of mammalian and Trypanosoma cruzi protein farnesyltransferase and Trypanosoma cruzi lanosterol-14-alpha-demethylase. [D] . Lockman, Jeffrey William. 2003

机译：设计，合成和具有药用价值的分子的生物学评估：哺乳动物和克鲁斯锥虫蛋白法尼基转移酶和克鲁斯锥虫羊毛甾醇14-α-脱甲基酶的抑制剂。
6. Mevinolin (lovastatin) potentiates the antiproliferative effects of ketoconazole and terbinafine against Trypanosoma (Schizotrypanum) cruzi: in vitro and in vivo studies. [O] . J A Urbina, K Lazardi, E Marchan, 1993

机译：Mevinolin（洛伐他汀）可增强酮康唑和特比萘芬对克氏锥虫的抗增殖作用：在体内和体外研究。
7. Mevinolin (lovastatin) potentiates the antiproliferative effects of ketoconazole and terbinafine against Trypanosoma (Schizotrypanum) cruzi: in vitro and in vivo studies. [O] . Urbina, J A, Lazardi, K, Marchan, E, 1993

机译：Mevinolin（洛伐他汀）可增强酮康唑和特比萘芬对克氏锥虫的抗增殖作用：在体内和体外研究。

5-Nitro-2-furyl derivative actives against Trypanosoma cruzi: preliminary in vivo studies.

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