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Antimicrobial activity of meta-alkoxyphenylcarbamates containing substituted N-phenylpiperazine fragment

机译:含取代的N-苯基哌嗪片段的间烷氧基苯基氨基甲酸酯的抗菌活性

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摘要

In the present investigation, the basic esters of meta-alkoxyphenylcarbamic acid bearing variously substituted N-phenylpiperazine fragment were screened for their in vitro antimicrobial activity against Staphylococcus aureus, Escherichia coli and Candida albicans, respectively. The most effective against Escherichia coli was found the compound 6d (MIC=195,3 μg/mL) bearing simultaneously para-fluoro substituent at the 4-phenylpiperazin-1-yl core and meta-methoxy side chain in the lipophilic part of the molecule. From whole analyzed set of the molecules the substance 8e with propoxy side chain forming meta-alkoxyphenylcarbamoyl fragment and lipophilic, sterically bulky meta-trifluoromethyl group attached at N-phenylpiperazine moiety was evaluated as the most active against Candida albicans (MIC=97,7 μg/mL). On the contrary, all investigated structures were practically inactive against Staphylococcus aureus (MIC>1000 μg/mL)
机译:在本研究中,对带有不同取代的N-苯基哌嗪片段的间烷氧基苯基氨基甲酸的碱性酯,分别针对金黄色葡萄球菌,大肠杆菌和白色念珠菌进行了体外抗菌活性筛选。发现对大肠杆菌最有效的化合物6d(MIC = 195,3μg/ mL)同时在分子的亲脂性部分的4-苯基哌嗪-1-基核心和间甲氧基侧链带有对氟取代基。从整个分子分析集中,将具有丙氧基侧链形成间烷氧基苯基氨基甲酰基片段和亲脂性,空间体积大的间三氟甲基连接在N-苯基哌嗪部分上的物质8e评估为对白色念珠菌最具活性的物质(MIC = 97.7μg / mL)。相反,所有研究的结构对金黄色葡萄球菌几乎没有活性(MIC> 1000μg/ mL)

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