Synthesis and antibacterial evaluation of certain quinolone derivatives
Synthesis and antibacterial evaluation of certain quinolone derivatives
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DOI：
10.1021/jm0100335
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发表时间：
2001-07-05
影响因子：
7.3
通讯作者：
Tzeng, CC
中科院分区：
文献类型：
--
作者：
Chen, YL;Fang, KC;Tzeng, CC
合成了一系列7位取代的喹诺酮衍生物，并对其抗菌活性和细胞毒活性进行了评价。初步结果表明，在这项研究中测试的大多数化合物表现出更好的抗耐甲氧西林金黄色葡萄球菌的活性比诺氟沙星。其中，1-（4-氨基-2-氟苯基）-6-氟-1，4-二氢-7-{4-[2-（4-甲氧苯基）-2-羟基亚氨基乙基]-1-哌嗪基}-4-氧代-3-喹啉羧酸（11 d）及其酮前体10 d对肺炎克雷伯菌、耐甲氧西林沙门氏菌、耐药沙门氏金黄色葡萄球菌、红霉素和氨苄青霉素耐药肺炎链球菌和万古霉素耐药粪肠球菌。由于lid的强细胞毒性（平均log GI（50）为-5.40），具有良好抗菌活性和低细胞毒性（平均log GI（50）为-4.67）的化合物10 d是更有潜力的候选药物。
A number of 7-substituted quinolone derivatives were synthesized and evaluated for antibacterial and cytotoxic activities. Preliminary results indicated that most compounds tested in this study demonstrated better activity against methicillin-resistant Staphylococcus aureus than norfloxacin. Among them, 1-(4-amino-2-fluorophenyl)-6-fluoro-1,4-dihydro-7-{4-[2-(4-methoxyphenyl)-2-hydroxyiminoethyl]-1-piperazinyl}-4-oxo-3-quinolinecarboxylic acid (11d) and its ketone precursor 10d exhibited significant activities against Klebsiella pneumoniae, methicillin-resistant S. aureus, erythromycin- and ampicillin-resistant Streptococcus pneumoniae, and vancomycin-resistant Enterococcus faecalis. Due to strong cytotoxicities of lid (a mean log GI(50) of -5.40), compound 10d, with good antibacterial activities and low cytotoxicities (a mean log GI(50) of -4.67), is a more potential drug candidate.