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某些新型2-(4-乙基-苯氧甲基)苯甲酸硫脲对浮游细胞的抗菌活性。

Antimicrobial activity of some new of 2-(4-ethyl-phenoximethyl) benzoic acid thioureides against planktonic cells.

作者信息

Drăcea Olguţa, Babeş Camelia, Limban Carmen, Delcaru Cristina, Chifiriuc Mariana Carmen, Israil Anca-Michaela

机构信息

National Institute of Research-Development for Microbiology and Immunology Cantacuzino, Spl. Independentei, 103, 050096 Bucharest, Romania.

出版信息

Roum Arch Microbiol Immunol. 2010 Apr-Jun;69(2):90-4.

Abstract

The aim of the present study was to evaluate the antimicrobial activity of new 2-(4-ethyl-phenoxymethyl) benzoic acid thioureides. The synthesis of the new compounds was done in three steps starting with the synthesis of 2-(4-ethyl-phenoxymethyl) benzoic acid. In the second stage, the 2-(4-ethyl-phenoxymethyl)-benzoyl chloride was prepared and the new thioureides were synthesized in the third step by the reaction of 2-(4-ethyl-phenoxymethyl) benzoyl isothiocyanate with various primary aromatic amines. The original compounds were screened for their in vitro antimicrobial activity against Gram-positive (Staphylococcus aureus, Bacillus subtilis) and Gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa) as well as to fungal strains (Candida albicans, Aspergillus niger), using both reference and clinical, multidrug resistant strains. The qualitative screening of the susceptibility spectra of various microbial strains versus these compounds was performed by three adaptated diffusion methods: (1) impregnation of the filter paper disks with the respective substance solutions, (2) distribution of the tested solutions into agar wells and (3) spotting of the respective solutions on the solid medium previously inoculated with the microbial suspensions. The quantitative assay of the antimicrobial activity was performed by broth microdilution method in 96-well microplates in order to establish the minimal inhibitory concentration (MIC). The tested compounds exhibited specific antimicrobial activity with MICs ranging from 3.9 microg/mL to 250 microg/mL.

摘要

本研究的目的是评估新型2-(4-乙基-苯氧基甲基)苯甲酸硫脲的抗菌活性。新化合物的合成分三步进行,首先合成2-(4-乙基-苯氧基甲基)苯甲酸。在第二阶段,制备2-(4-乙基-苯氧基甲基)苯甲酰氯,并在第三步通过2-(4-乙基-苯氧基甲基)苯甲酰异硫氰酸酯与各种伯芳香胺反应合成新的硫脲。使用参考菌株和临床多药耐药菌株,对原始化合物针对革兰氏阳性菌(金黄色葡萄球菌、枯草芽孢杆菌)、革兰氏阴性菌(大肠杆菌、肺炎克雷伯菌、铜绿假单胞菌)以及真菌菌株(白色念珠菌、黑曲霉)的体外抗菌活性进行筛选。通过三种改进的扩散方法对各种微生物菌株对这些化合物的药敏谱进行定性筛选:(1) 用相应物质溶液浸渍滤纸圆盘;(2) 将测试溶液分布到琼脂孔中;(3) 将相应溶液点样在预先接种微生物悬液的固体培养基上。通过在96孔微孔板中采用肉汤微量稀释法进行抗菌活性的定量测定,以确定最低抑菌浓度(MIC)。测试的化合物表现出特定的抗菌活性,MIC范围为3.9微克/毫升至250微克/毫升。

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