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首页> 外文期刊>The Journal of Antibiotics: An International Journal >In vitro and in vivo anti-Trypanosoma brucei activities of phenazinomycin and related compounds
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In vitro and in vivo anti-Trypanosoma brucei activities of phenazinomycin and related compounds

机译:苯那霉素和相关化合物的体外和体内抗布鲁氏锥虫活性

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During the course of our screening program to discover new antitrypanosomal compounds, we have evaluated isolates from soil microorganisms as well as compounds from the antibiotic libraries of the Kitasato Institute for Life Sciences and Bioscience Associates. We have previously reported on various microbial metabolites exhibiting potent anti-Trypanosoma brucei properties, which are defined as antitrypanosomal properties. We have recently evaluated the known phena-zine antibiotics, phenazinomycin, griseoluteic acid, griseolutein В and related compounds, some of which have shown significant antitrypanosomal activities, both in vitro and in vivo. Here, we report the antitrypanosomal profiles of phenazinomycin and some related compounds (Figure 1) in comparison with those of some clinically used antitrypanosomal drugs, such as suramin and eflornithine. We also present our findings with respect to structure-activity relationships.
机译:在我们的筛选程序中,发现了新的抗锥虫类化合物,我们评估了来自土壤微生物的分离株以及北里生命科学研究院和生物科学协会的抗生素文库中的化合物。我们以前曾报道过各种表现出有效的抗布鲁氏锥虫特性的微生物代谢产物,这些特性被定义为抗锥虫特性。我们最近评估了已知的苯甲嗪类抗生素,苯那霉素,灰黄酸,灰黄素®和相关化合物,其中一些在体外和体内均显示出显着的抗锥虫活性。在这里,我们报告了苯那霉素和一些相关化合物(图1)与一些临床使用的抗胰蛋白drugs药物(如苏拉明和弗洛尼丁)的抗胰蛋白profiles谱(图1)。我们还介绍了关于结构-活性关系的发现。

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