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Design and Synthesis of 3,6-Disubstituted- and 2,3,6-Trisubstitutedquinoxalines: Docking and In Vitro Antimicrobial Study
Polycyclic Aromatic Compounds ( IF 2.4 ) Pub Date : 2020-06-18 , DOI: 10.1080/10406638.2020.1781210
Magda M. F. Ismail 1 , Hend M. A. El-Sehrawi 1 , Maha M. Khalifa 1 , Marwa F. Harras 1
Affiliation  

Abstract

Antimicrobial chemotherapy is the clinical application of antimicrobial agents to treat infectious disease. A new series of 3,6-disubstituted- and 2,3,6-trisubstitutedquinoxalines have been synthesized by appropriate methods. All test compounds have been evaluated for in vitro antimicrobial activity. Further investigation using MIC experiment was performed; It appears that, compound 14c has higher broad-spectrum antibacterial activity (MIC= 0.01–0.24 ug/ml) than the reference drug, streptomycin (MIC= 0.03–0.97 ug/ml). As well, it elicited remarkable antifungal activity than the reference drug clotrimazole against almost all the selected strains. Moreover, docking study of the most active compounds into MurF active site has confirmed their binding affinity to MurF.



中文翻译:

3,6-二取代和 2,3,6-三取代喹喔啉的设计和合成:对接和体外抗菌研究

摘要

抗菌化学疗法是抗菌药物治疗感染性疾病的临床应用。通过适当的方法合成了一系列新的 3,6-二取代和 2,3,6-三取代喹喔啉。所有测试化合物都经过体外抗微生物活性评估。使用MIC实验进行了进一步调查;看来,化合物14c的广谱抗菌活性 (MIC= 0.01–0.24 ug/ml) 高于参考药物链霉素 (MIC= 0.03–0.97 ug/ml)。同样,它对几乎所有选定的菌株都比参考药物克霉唑具有显着的抗真菌活性。此外,最活跃的化合物与MurF活性位点的对接研究证实了它们与MurF的结合亲和力。

更新日期:2020-06-18
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