首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, structure and biological activity of pseudopeptidic macrolides based on an amino alcohol.
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Synthesis, structure and biological activity of pseudopeptidic macrolides based on an amino alcohol.

机译:基于氨基醇的拟肽大环内酯类化合物的合成,结构和生物学活性。

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摘要

A series of new pseudopeptidic macrolides 2a-f based on an amino alcohol were synthesized and evaluated for in vitro antibacterial and antifungal activities. The structure-activity relationships of these compounds were studied and the results showed that compounds 2a and 2d exhibited moderate antibacterial activity against Staphylococcus aureus, Bacillus subtilis and Escherichia coli, whereas compound 2e showed potent antifungal activity against all the fungal species tested, showing a promising broad-spectrum antifungal activity. All the compounds have been studied in vitro for the hemolytic activity as a measure of their cytotoxicity, showing that these compounds have low lytic properties.
机译:合成了一系列基于氨基醇的新型伪肽类大环内酯2a-f,并对其体外抗菌和抗真菌活性进行了评估。研究了这些化合物的构效关系,结果表明化合物2a和2d对金黄色葡萄球菌,枯草芽孢杆菌和大肠杆菌具有中等程度的抗菌活性,而化合物2e对所有测试的真菌种类均具有有效的抗真菌活性。广谱抗真菌活性。已经对所有化合物的溶血活性进行了体外研究,以此来衡量它们的细胞毒性,表明这些化合物具有较低的裂解特性。

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