首页> 外文期刊>Journal of Microbiology, Biotechnology and Food Sciences >THE IN VITRO EVALUATION OF ortho-/meta-/para-ALKOXYPHENYLCARBAMIC ACID ESTERS BEARING 4-(2-FLUORO-/2-METHYLPHENYL)PIPERAZIN-1-YL MOIETY AGAINST MYCOBACTERIUM TUBERCULOSIS H37Ra STRAIN
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THE IN VITRO EVALUATION OF ortho-/meta-/para-ALKOXYPHENYLCARBAMIC ACID ESTERS BEARING 4-(2-FLUORO-/2-METHYLPHENYL)PIPERAZIN-1-YL MOIETY AGAINST MYCOBACTERIUM TUBERCULOSIS H37Ra STRAIN

机译:结核分枝杆菌H37Ra菌株4-(2-氟-/ 2-甲基苯基)哌嗪-1-基部分-邻-/间-/对-烷氧基苯甲酸甲酯的体外评价

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摘要

In a continual research of ortho-/meta-/para-alkoxyphenylcarbamic acid esters as antimycobacterially active compounds, the purpose of current paper was to in vitro screen the potency of the molecules containing incorporated substituted N-phenylpiperazin-1-yl moiety against attenuated M. tuberculosis H37Ra strain which was grown in Middlebrook broth, supplemented with Oleic-Albumin-Dextrose- Catalase supplement and mycobactin J (2 μg/mL) as well. The susceptibility of concerned mycobacterial strain was investigated in a 96-well plate format, the plates were incubated at 37°C for 7 days. According to minimum inhibitory concentrations, as the lowest concentrations which prevented a visual colour change, it was observed that positional ortho-/meta-/para-alkoxy side chain isomerism as well as high lipophilicity did not decisively influenced the effectiveness of inspected compounds. Moreover, qualitatively different substitution within basic compartment in terms of electronic properties and possible hydrophobic interactions did not lead to the improvement in the activity.
机译:在对作为抗分枝杆菌活性化合物的邻-/间-/对-烷氧基苯基氨基甲酸酯的持续研究中,当前论文的目的是体外筛选包含掺入的取代N-苯基哌嗪-1-基部分的分子对减毒M的效力在Middlebrook肉汤中生长的结核H37Ra菌株,还补充了油酸-白蛋白-葡萄糖-过氧化氢酶补充剂和霉菌素J(2μg/ mL)。以96孔板形式研究了相关分枝杆菌菌株的敏感性,将板在37℃下孵育7天。根据最小抑制浓度,作为防止视觉颜色变化的最低浓度,观察到位置邻-/间-/对-烷氧基侧链异构以及高亲脂性不会决定性地影响所检查化合物的有效性。而且,就电子性质和可能的疏水相互作用而言,基本部分内在质上的不同取代没有导致活性的提高。

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