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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Novel depsides as potential anti-inflammatory agents with potent inhibitory activity against Escherichia coli-induced interleukin-8 production
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Novel depsides as potential anti-inflammatory agents with potent inhibitory activity against Escherichia coli-induced interleukin-8 production

机译:新型潜在的抗炎药,对大肠杆菌诱导的白介素8的产生具有潜在的抑制作用

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摘要

Sixteen novel depsides were synthesized for the first time. Their chemical structures were clearly determined by 1H NMR, ESI mass spectra, and elemental analyses. All the compounds were assayed for antibacterial activities against three Gram-positive bacterial strains (Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6538, and Streptococcus faecalis ATCC 9790) and three Gram-negative bacterial strains (Escherichia coli ATCC 35218, Pseudomonas aeruginosa ATCC 13525, and Enterobacter cloacae ATCC 13047) by the MTT method. Compound 2-(2-methoxy-2-oxoethyl)phenyl 5-bromonicotinate (5) exhibited significant antibacterial activities against E. coli ATCC 35218 with an MIC of 0.78 μg/mL, which was superior to the positive control kanamycin B. In addition, compound 5 showed potent inhibitory activity against E. coli-induced interleukin-8 production.
机译:首次合成了十六种新颖的多肽。通过1H NMR,ESI质谱和元素分析清楚地确定了它们的化学结构。测定了所有化合物对三种革兰氏阳性细菌菌株(枯草芽孢杆菌ATCC 6633,金黄色葡萄球菌ATCC 6538和粪链球菌ATCC 9790)和三种革兰氏阴性细菌菌株(大肠杆菌ATCC 35218,铜绿假单胞菌ATCC 13525)的抗菌活性MTT法测定阴沟肠杆菌(ATCC 13047)。化合物2-(2-甲氧基-2-氧乙基)苯基5-溴烟酸酯(5)对大肠杆菌ATCC 35218表现出显着的抗菌活性,MIC为0.78μg/ mL,优于阳性对照卡那霉素B.化合物5显示出对大肠杆菌诱导的白介素8产生的有效抑制活性。

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