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Synthesis and Antimicrobial Evaluation of Novel Polyfused Heterocycles-Based Quinolone

机译:新型基于杂环的稠合杂环喹诺酮的合成与抗菌评价

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摘要

Syntheses of some new heterocyclic compounds incorporating quinolone moieties were achieved via reaction of 4-hydroxy-7-methoxyquinolin-2(1H)-one (1) or 3-bromo-4-hydroxy-7-methoxyquinolin-2(1H)-one (2) with binucleophilic reagents. The newly synthesized compounds were characterized by elemental analyses and spectral data (IR, H-1-NMR and mass spectra). The newly synthesized compounds were screened for their antibacterial activity against Gram-positive bacteria (Bacillus thuringiensis) and Gram-negative bacteria (Escherichia coli). The results showed clearly that compounds 1 and 3 are the more potent antibacterial agents against E. coli, compounds 4, 5, 6 and 8, 9, 10, 11, 12, 13 exhibited moderate activities against E. coli strain, and compounds 7 and 11 exhibited weak activities compared with Gentamicin as a well known standard drug.
机译:通过4-羟基-7-甲氧基喹啉-2(1H)-一(1)或3-溴-4-羟基-7-甲氧基喹啉-2(1H)-一的反应,实现了一些新的并入喹诺酮部分的杂环化合物的合成。 (2)用双亲试剂。通过元素分析和光谱数据(IR,H-1-NMR和质谱)对新合成的化合物进行了表征。筛选新合成的化合物对革兰氏阳性细菌(苏云金芽孢杆菌)和革兰氏阴性细菌(大肠杆菌)的抗菌活性。结果清楚地表明,化合物1和3是对大肠杆菌更有效的抗菌剂,化合物4、5、6和8、9、10、11、12、13对大肠杆菌菌株具有中等活性,化合物7与庆大霉素(一种众所周知的标准药物)相比,其11和11的活性较弱。

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