首页> 外文期刊>Quimica nova >Synthesis and preliminary evaluation of n-acylhydrazone compounds as antibacterial and antifungal agents [Síntese e avalia??o preliminar da atividade antibacteriana e antifúngica de derivados N-acilidraz?nicos]
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Synthesis and preliminary evaluation of n-acylhydrazone compounds as antibacterial and antifungal agents [Síntese e avalia??o preliminar da atividade antibacteriana e antifúngica de derivados N-acilidraz?nicos]

机译:N-酰基hydr化合物作为抗菌和抑菌剂的合成与初步评价[N-酰基肼衍生物的合成及抗菌活性的初步评价]

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摘要

We describe the synthesis and evaluation of N-acylhydrazone compounds bearing different electron-donating groups in one of its aromatic rings, obtained using a four-step synthetic route. IC50 values against pathogenic fungi and bacteria were determined by serial microdilution. Compounds showed low activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. By contrast, a derivative with a meta-oriented electron-donating group showed significant activity (IC50) against Candida albicans (17 mM), C. krusei (34 mM) and C. tropicalis (17 mM). Results suggest this is a promising lead-compound for synthesis of potent antifungal agents.
机译:我们描述了合成和评估的N-酰基hydr化合物在其芳香环之一中带有不同的供电子基团,采用四步合成途径获得。通过连续微量稀释确定针对致病性真菌和细菌的IC50值。化合物对金黄色葡萄球菌,大肠杆菌和铜绿假单胞菌的活性较低。相比之下,具有间位给电子基团的衍生物显示出对白色念珠菌(17 mM),克鲁氏梭菌(34 mM)和热带梭菌(17 mM)的显着活性(IC50)。结果表明,这是用于合成有效抗真菌剂的有前途的铅化合物。

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