New Conjugates of Quinoxaline as Potent Antitubercular and Antibacterial Agents

R. Peraman, R. Kuppusamy, Sunil Kumar Killi, Y. P. Reddy
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引用次数: 21

Abstract

Considering quinoxaline as a privileged structure for the design of potent intercalating agents, some new sugar conjugates of quinoxaline were synthesized and characterized by IR, 1HNMR, 13C NMR, and mass spectral data. In vitro testing for antitubercular and antimicrobial activities was performed against Mycobacterium tuberculosis H 37 Rv and some pathogenic bacteria. Results revealed that conjugate containing ribose moiety demonstrated the most promising activity against Mycobacteria and bacteria with minimum inhibitory concentrations (MIC) of 0.65 and 2.07 μM, respectively. Other conjugates from xylose, glucose, and mannose were moderately active whilst disaccharides conjugates were found to be less active. In silico docking analysis of prototype compound revealed that ATP site of DNA gyrase B subunit could be a possible site for inhibitory action of these synthesized compounds.
喹诺啉的新结合物作为有效的抗结核和抗菌药物
考虑到喹啉是设计强插层剂的有利结构,合成了一些新的喹啉糖偶联物,并通过IR、1HNMR、13C NMR和质谱数据对其进行了表征。对结核分枝杆菌h37rv和部分致病菌进行了体外抗结核和抗菌活性试验。结果表明,含有核糖片段的缀合物对分枝杆菌和细菌的最低抑制浓度(MIC)分别为0.65 μM和2.07 μM,具有较好的抑制活性。木糖、葡萄糖和甘露糖的其他偶联物具有中等活性,而双糖偶联物活性较低。原型化合物的硅对接分析表明,DNA回转酶B亚基的ATP位点可能是这些合成化合物抑制作用的可能位点。
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期刊介绍: International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis. International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis.
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