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

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.