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Synthesis, Characterization, Biocomputational Modeling and Antibacterial Study of Novel Pyran Based on 8-Hydroxyquinoline
Arabian Journal for Science and Engineering ( IF 2.6 ) Pub Date : 2020-11-16 , DOI: 10.1007/s13369-020-05089-y
M. Rbaa , A. Hichar , P. Dohare , El H. Anouar , Y. Lakhrissi , B. Lakhrissi , M. Berredjem , F. Almalki , V. Rastija , M. Rajabi , T. Ben Hadda , A. Zarrouk

In this work, we report the synthesis of a new family of organic compounds based on 8-hydroxyquinoline using a simple and efficient method. The synthesized 8-hydroxyquinoline derivatives were characterized by analysis of 1H and 13C NMR, FT-IR spectral data and elemental analysis (EA). Their antibacterial activity is tested against Gram-positive strains [S. aureus (ATCC29213), V. parahaemolyticus (ATCC17802)] and Gram negative [E. coli (ATCC35218), P. aeruginosa (ATCC27853)] by the use of the agar diffusion technique. The obtained results showed that the synthesized 8-hydroxyquinoline derivatives have a potent antibacterial activity against the tested strains compared to Norfloxacin as a standard antibiotic. The results also reveal the effectiveness of these compounds at low concentrations, with a MIC of 1.00 μg/ml for compound 4a. Their antibacterial activity has also been optimized by bioinformatics studies (POM analyses). The experimental results are in relatively good agreement with the corresponding theoretical ones.



中文翻译:

基于8-羟基喹啉的新型吡喃的合成,表征,生物计算模型和抗菌研究

在这项工作中,我们报告了一种使用简单有效的方法合成基于8-羟基喹啉的有机化合物的新家族。通过1 H和13 C NMR分析,FT-IR光谱数据和元素分析(EA)对合成的8-羟基喹啉衍生物进行了表征。测试了它们对革兰氏阳性菌株[金黄色葡萄球菌(ATCC29213),副溶血性弧菌(ATCC17802)]和革兰氏阴性菌株[大肠杆菌(ATCC35218),铜绿假单胞菌]的抗菌活性(ATCC27853)],使用琼脂扩散技术。获得的结果表明,与作为标准抗生素的诺氟沙星相比,合成的8-羟基喹啉衍生物对被测菌株具有有效的抗菌活性。结果还揭示了这些化合物在低浓度下的有效性,化合物4a的MIC为1.00μg/ ml 。它们的抗菌活性也已通过生物信息学研究(POM分析)进行了优化。实验结果与理论值比较吻合。

更新日期:2020-11-16
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