Synthesis and antibacterial activity of the 4-quinolone-3-carboxylic acid derivatives having a trifluoromethyl group as a novel n-1 substituent
Synthesis and antibacterial activity of the 4-quinolone-3-carboxylic acid derivatives having a trifluoromethyl group as a novel n-1 substituent
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DOI：
10.1021/jm040204g
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发表时间：
2005-05-05
影响因子：
7.3
通讯作者：
Ishizaki, T
中科院分区：
文献类型：
--
作者：
Asahina, Y;Araya, I;Ishizaki, T
合成了新的1-三氟甲基-4-喹诺酮类化合物（8a，B），并对其抗菌活性进行了评价。采用氧化酯化-缩合反应在N-1位引入三氟甲基作为关键步骤。在这些衍生物中，发现8a对金黄色葡萄球菌Smith、肺炎链球菌IID 1210和大肠杆菌NIHJ JC-2表现出与诺氟沙星（1）相当的抗菌活性。
Novel 1-trifluoromethyl-4-quinolone derivatives (8a,b) were synthesized, and the antibacterial activity of each was evaluated. An oxidative desulfarization-fluorination reaction was employed to introduce a trifluoromethyl group at the N-1 position as a key step. Among the derivatives, 8a was found to exhibit antibacterial activity comparable to that of norfloxacin (1) against Staphylococcus aureus Smith, Streptococcus pneumoniae IID1210, and Escherichia coli NIHJ JC-2.