新型氟喹诺酮类似物的合成及抗菌活性  

Synthesis and Antibacterial Activities of Novel Fluoroquinolone Derivatives

作　　者：陈修华 刘丽君 黄朝漫 张应烙 李新生[1] CHEN Xiu-hua;LIU Li-jun;HUANG Chao-man;ZHANG Ying-lao;LI Xin-sheng(College of Chemistry and Life Sciences,Zhejiang Normal University,Jinhua 321000,China;College of Life Sciences,Anhui Agricultural University,Hefei 230036,China)

机构地区：[1]浙江师范大学化学与生命科学学院,浙江金华321004 [2]安徽农业大学生命科学学院,安徽合肥230036

出　　处：《合成化学》2021年第8期661-666,共6页Chinese Journal of Synthetic Chemistry

摘　　要：通过氢解,偶联及浓盐酸脱保护合成了10种新型的氟喹诺酮衍生物(A1~A6,B1~B4),总收率50%~65%,其结构经^(1)H NMR,^(13)C NMR和MS(ESI)表征。测定了目标化合物对大肠杆菌、金黄色葡萄球菌和四联球菌的抗菌活性。结果表明:目标化合物对3种供试细菌均有良好的抑制效果,其中化合物A1和A2对金黄色葡萄球菌和大肠杆菌抑制效果最好,微弱于左氧氟沙星;A5对四联球菌的抑制效果优于左氧氟沙星。Ten novel fluoroquinolone derivatives(A1~A6,B1~B4)were synthesized with a total yield of 50%~65%by hydrogenolysis,coupling and deprotection reaction.The target compounds are characterized by ^(1)H NMR,^(13)C NMR and MS(ESI).The antibacterial activity of the ten compounds against Escherichia coli,Staphylococcus aureus and Micrococcus tetragenus was researched.The results showed the ten compounds possessed good activity against three tested bacteria.Among the ten compounds,A1 possessed the most potent activity against S.aureus,A2 possessed the most potent activity against E.coli,and the antibacterial activities of A1 and A2 is weaker than that of levofloxacin;A5 possessed the most potent activity against M.tetragenus,and the antibacterial activity of A5 against M.tetragenus is better than that of levofloxacin.

关 键 词：氟喹诺酮 合成 抗菌活性 大肠杆菌 金黄色葡萄球菌 四联球菌 偶联 氢解 

分 类 号：O626.13[理学—有机化学]