Wang H, Qi J, Sun L, Yu L, Guo H
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050.
Yao Xue Xue Bao. 1998 Sep;33(9):675-81.
Eighteen pyridonecarboxylic acids, characterized by a methyl group at the C6-position instead of the usual fluorine atom, cyclopropyl at the N1-position, substituted amino groups at the C7-position, and some substituted groups (hydrogen, chlorine, nitro and amino) at the C8-position, were synthesized. The in vitro antibacterial activity of these compounds were tested, and the structure-activity relationships were also discussed. The results of the study showed that the activity of compounds 22 and 24 were less potent than that of ciprofloxacin against S. aureus, S. epidermidis, E. coli and P. aeruginosa, while they were 2-100 times more potent than ciprofloxacin against K. pneumoniae, S. marcescens, A. calcoacetous, E. aerogenes, S. typhi and S. typhimurium.
合成了18种吡啶酮羧酸，其特征在于C6位为甲基而非通常的氟原子，N1位为环丙基，C7位为取代氨基，C8位有一些取代基（氢、氯、硝基和氨基）。测试了这些化合物的体外抗菌活性，并讨论了构效关系。研究结果表明，化合物22和24对金黄色葡萄球菌、表皮葡萄球菌、大肠杆菌和铜绿假单胞菌的活性比环丙沙星弱，而对肺炎克雷伯菌、粘质沙雷氏菌、产碱杆菌、产气肠杆菌、伤寒沙门氏菌和鼠伤寒沙门氏菌的活性比环丙沙星强2至100倍。
