Synthesis and Evaluation of Antibacterial Activity of Novel Disubstituted 1,3,4-Oxadiazoles Derivatives Containing Fluorine Substituent

A. Souldozi
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Abstract

In the present study a new series of antibacterial agents (4a-f) was designed, synthesized and evaluated for antibacterial activity against different gram positive (Staphylococcusaureus, Staphylococcus epidermidis, Bacillus cereus) and gram negative (listeria monocytogenes, Escherichia coli, Pseudomonas aeroginosa) bacteria. New derivatives of oxadiazoles were prepared by one-pot reaction of N-isocyanoiminotriphenylphosphorane, carboxylic acid derivatives and 2-pyridinecarboxaldehyde, in the presence of acetonitrile solvent. The broth macro dilution and well agar diffusion methods were used for determination of inhibition zone (IZ) and minimum inhibitory concentration (MIC) during preliminary evaluation of antimicrobial activity. The (MIC) values of tested compounds revealed that all compounds have displayed significant antibacterial activity against Staphylococcusaureus and Staphylococcus epidermidis (with MIC values in the range of 31 to 125µg/mL).
含氟取代基的新型二取代 1,3,4-恶二唑衍生物的合成及其抗菌活性评估
本研究设计、合成了一系列新的抗菌剂(4a-f),并评估了它们对不同革兰氏阳性菌(金黄色葡萄球菌、表皮葡萄球菌、蜡样芽孢杆菌)和革兰氏阴性菌(单核细胞增生李斯特氏菌、大肠杆菌、绿脓杆菌)的抗菌活性。在乙腈溶剂存在下,N-异氰基亚氨基三苯基膦、羧酸衍生物和 2-吡啶甲醛发生一锅反应,制备出新的噁二唑衍生物。在初步评估抗菌活性时,采用肉汤宏观稀释法和井琼脂扩散法测定抑菌区(IZ)和最低抑菌浓度(MIC)。测试化合物的 MIC 值显示,所有化合物都对金黄色葡萄球菌和表皮葡萄球菌具有显著的抗菌活性(MIC 值范围在 31 至 125µg/mL 之间)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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