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目的设计、合成系列新型氟喹诺酮类衍生物,并初筛其体外抗菌活性。方法通过酰胺键在洛美沙星、左氧氟沙星和加替沙星的C-7位引入乙酰基、正己酰基、苯乙酰基和三甲氧基苯乙酰基,制备了一系列氟喹诺酮类衍生物,并通过二倍稀释法进行抗菌活性初筛。结果与讨论共制备12个全新目标物,结构经1HNMR、13CNMR和HRMS确证。通过对金黄色葡萄球菌、大肠埃希菌和铜绿假单胞菌的体外抗菌活性初筛,发现化合物7的抗菌活性优于阳性对照。此外,在C-7位引入乙酰基的化合物7~9的抗菌活性显著优于母核相同、C-7侧链不同的结构类似物。
Aim To design and synthesize a series of novel fluoroquinolone derivatives and to screen their antibacterial activity in vitro. Methods A series of fluoroquinolone derivatives were prepared by introducing acetyl, n-hexanoyl, phenylacetyl and trimethoxyphenylacetyl groups at the C-7 position of lomefloxacin, levofloxacin and gatifloxacin through amide bonds, Two-fold dilution of antibacterial activity of screening. Results and Discussion A total of 12 new targets were prepared and the structures were confirmed by 1HNMR, 13CNMR and HRMS. Through in vitro screening of Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa, the antibacterial activity of compound 7 was better than that of positive control. In addition, the antibacterial activity of compounds 7 to 9, which introduced acetyl group at C-7 position, was significantly better than that of the same structural part of mother nucleus and different structural side chain of C-7.