新型喹诺酮类化合物的合成及抗菌活性研究  

Synthesis and antibacterial activity of a series of new quinolones

作　　者：臧英博 苏楠 安然 苏昕[2] 郭春[1] ZANG Ying-bo;SU Nan;AN Ran;SU Xin;GUO Chun(School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China;School of Life Sciences and Biopharmaceuticals,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]沈阳药科大学生命科学与生物制药学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2021年第5期329-336,共8页Chinese Journal of Medicinal Chemistry

摘　　要：目的设计、合成一系列新型喹诺酮类化合物,测试其体外抗菌活性。方法以诺氟沙星为起始原料,经过N-烃化、酰化和缩合共3步反应得到目标化合物,采用微量二倍浓度稀释法,以诺氟沙星、环丙沙星、左氧氟沙星为阳性对照测定目标化合物对金黄色葡萄球菌、枯草芽孢杆菌、铜绿假单胞菌、大肠杆菌、肺炎克雷伯菌的体外抑菌活性。结果与结论合成了22个喹诺酮类衍生物,目标化合物的结构经1H-NMR和HR-MS谱确证。体外抗菌活性测试结果表明,大多数目标化合物对多种测试细菌显示出不同程度的抑制活性,其中3个化合物3、6、14的活性优于阳性对照药左氧氟沙星,具有进一步研究的潜质,为新型喹诺酮类抗菌药物的研究奠定了基础。In order to discover drugs with higher antibacterial activity, a series of quinolone compounds were designed and synthesized, and their antibacterial activities in vitro were evaluated primarily.Twenty-two target compounds were synthesized from norfloxacin by N-alkylation, acylation and condensation reactions, and their structures were confirmed by 1H-NMR and HR-MS.The antibacterial activities of the target compounds against Staphylococcus aureus,Bacillus subtilis,Pseudomonas aeruginosa,Escherichia coli and Klebsiella pneumoniae were determined by MIC test.Most of the target compounds showed different degrees of inhibitory activity against a variety of testing bacteria.Compounds 3,6 and 14 exhibited higher antibacterial activity than levofloxacin and have the potential for further research, which provide a basis for the research of new quinolone antibacterial drugs.

关 键 词：喹诺酮 杂合物 抗菌活性 

分 类 号：R914[医药卫生—药物化学]