Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Bratislava, Slovak Republic.
Braz J Microbiol. 2013 Oct 30;44(2):457-63. doi: 10.1590/S1517-83822013000200018. eCollection 2013.
In current research, nine basic esters of para-alkoxyphenylcarbamic acid with incorporated 4-(4-fluoro-/3-trifluoromethylphenyl)piperazin-1-yl fragment, 6i-6m and 8f-8i, were screened for their in vitro antimicrobial activity against Candida albicans, Staphylococcus aureus and Escherichia coli, respectively. Taking into account the minimum inhibitory concentration assay (MIC), as the most active against given yeast was evaluated 8i (MIC = 0.20 mg/mL), the most lipophilic structure containing para-butoxy and trifluoromethyl substituents. Investigating the efficiency of the compounds bearing only a single atom of fluorine and appropriate para-alkoxy side chain against Candida albicans, the cut-off effect was observed. From evaluated homological series, the maximum of the effectiveness was noticed for the stucture 6 k (MIC = 0.39 mg/mL), containing para-propoxy group attached to phenylcarbamoyloxy fragment, beyond which the compounds ceased to be active. On the contrary, all the tested molecules were against Staphylococcus aureus and Escherichia coli (MICs > 1.00 mg/mL) practically inactive.
在当前的研究中,筛选了 9 种带有 4-(4-氟-/3-三氟甲基苯基)哌嗪-1-基片段的对烷氧基苯基氨基甲酸酯的基本酯,即 6i-6m 和 8f-8i,以评估它们对白色念珠菌、金黄色葡萄球菌和大肠杆菌的体外抗菌活性。考虑到最低抑菌浓度测定(MIC),评估了对给定酵母最具活性的 8i(MIC = 0.20 mg/mL),其具有最多脂溶性结构,含有对丁氧基和三氟甲基取代基。研究了仅含有一个氟原子和适当的对烷氧基侧链的化合物对白色念珠菌的效率,观察到截止效应。在所评估的同源系列中,对含有连接到苯氨基甲酰氧基片段的对丙氧基基团的结构 6k 注意到最大的效果(MIC = 0.39 mg/mL),超过该化合物就不再具有活性。相反,所有测试的分子对金黄色葡萄球菌和大肠杆菌(MICs > 1.00 mg/mL)几乎没有活性。