三环氟喹诺酮类化合物的合成及抗菌活性

SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF TRICYCIC FLUOROQUINOLONES

摘要: 芦氟沙星(Rufloxacin)是氟喹诺酮类抗菌药物,由于它在体内有高效、广谱、长效和口服吸收良好等特点,我们在保留芦氟沙星母核基本骨架的基础上进行结构修饰,合成了12个新化合物。体外抑菌试验发现随着10位边链的极性增大,对革兰氏阴性(G^-)菌的抗菌活性增强,而对革兰氏阳性(G⁺)菌活性则变化不大。

Abstract: Twelve new analogues of new tricyclic rufloxacin were prepared and their MIC were evaluated against thirteen kinds of bacteria. As a result of these studies: the polarity of C₁₀-side chain was found to exert greater positive effect on G^- than on G⁺ bactria.