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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Antimicrobial Activity of Substituted Benzopentathiepin-6-amines
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Antimicrobial Activity of Substituted Benzopentathiepin-6-amines

机译：取代苯并戊脂素-6-胺的抗菌活性

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摘要

A number of substituted benzopentathiepin-6-amines and their analogues without a polysulfur ring were synthesized and evaluated in vitro for antimicrobial activity against a panel of reference bacterial and fungal strains. Trifluoroacetamide 14 demonstrated high antibacterial activity against Staphylococcus aureus (MRSA strain) with a MIC of 4 mu g/mL, which was four-fold higher than the activity of a reference drug amoxicillin. This compound was also most active against the Candida albicans fungus (MIC of 1 mu g ml(-1)), whereas amide 17 containing a morpholine substituent was most active against the Cryptococcus neoformans fungus (MIC of 2 mu g ml(-1)). These compounds have no hemolytic activity and are low cytotoxic. Replacement of the pentathiepine ring with 1,3-dithiolan-2-one or 1,3-dithiolane moieties leads to loss of antimicrobial activity. Based on the QSAR analysis and molecular docking data, bacterial DNA ligase might be one of the targets for the antibacterial activity of substituted benzopentathiepin-6-amines against S. aureus.
机译：合成了许多取代的苯并肠道蛋白-6-胺及其在没有多硫脲环的类似物，并在体外进行抗微生物活性对参考细菌和真菌菌株进行抗微生物活性。三氟乙酰胺14对金黄色葡萄球菌（MRSA菌株）的高抗菌活性具有4μg/ ml的MIC，其比参考药物阿莫西林的活性高四倍。该化合物对念珠菌（-1）的念珠菌（-1）的念珠菌（-1））的念珠菌（MIC）最活跃，而含有吗啉取代基的酰胺17对碱性蛋白质芳烃（MIC为2μgml（-1） ）。这些化合物没有溶血活性，并且是低细胞毒性的。用1,3-二硫醇-2-一或1,3-二硫醇部分替换近硫代哌环戒指导致抗菌活性的丧失。基于QSAR分析和分子对接数据，细菌DNA连接酶可能是取代的苯齐匹皮达病吡喃-6-胺对抗金黄色葡萄球菌的抗菌活性的靶标的靶标。

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