Li X H, Tian Z M, Miao H, Yu L X, Guo H Y
Institute of Medicinal Biotechnology, Chinese Acadeny of Medical Sciences, Peking Union Medical College, Beijing 100050.
Yao Xue Xue Bao. 1997 Nov;32(11):844-51.
Sixteen pyridonecarboxylic acids, characterized by having a chlorine atom and a cyclopropyl group at the 6- and 1-position respectively, substituted amino groups at the 7-position, and some substituted groups (chloro, nitro, amino, dimethylamino) at the 8-position, were synthesized. In vitro antibacterial activities of these compounds were tested. The fluoroquinolones ciprofloxacin and norfloxacin were included for comparative purposes. The results showed that both 11 Ca and 11 Cc were 4-8 times more active than ciprofloxacin and norfloxacin against S. aureus-15 in vitro, but with the same activity as ciprofloxacin against E. coli-22 and P. aeruginosa-29.
合成了16种吡啶酮羧酸，其特征在于分别在6位和1位具有氯原子和环丙基，在7位具有取代氨基，在8位具有一些取代基（氯、硝基、氨基、二甲氨基）。测试了这些化合物的体外抗菌活性。为作比较纳入了氟喹诺酮类药物环丙沙星和诺氟沙星。结果表明，11Ca和11Cc在体外对金黄色葡萄球菌-15的活性比环丙沙星和诺氟沙星高4至8倍，但对大肠杆菌-22和铜绿假单胞菌-29的活性与环丙沙星相同。
