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Design, Synthesis and Antibacterial Evaluation of 1-[(1R,2S)-2-Fluorocyclopropyl]ciprofloxacin-1,2,4-triazole-5(4H)-thione Hybrids

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机构: [a]Xuanwu Hospital, Capital Medical University, Beijing 100053, P. R. China [b]Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, P. R. China, [c]HuangHuai University, Zhumadian 463000, P. R. China [d]Pony Testing International Group Co. Ltd. (Wuhan), Wuhan 430034, P. R. China,
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关键词: quinolone ciprofloxacin 1 2 4-triazole-5(4H)-thione antibacterial activities structure-activity relationship

摘要:
A new class of 1-[(1R,2S)-2-fluorocyclopropyl]ciprofloxacin (CPFX)-1,2,4-triazole-5(4H)-thione hybrids 6a-6o was designed, synthesized and evaluated for their invitro antibacterial activities against a panel of clinically important drug-sensitive and drug-resistant Gram-positive and Gram-negative pathogens. Our results revealed that all hybrids 6a-6o had great potency against the tested strains, especially Gram-negative pathogens. The synthesized hybrids were more potent than the parent 1-[(1R,2S)-2-fluorocyclopropyl]CPFX (1) and comparable to CPFX and levofloxacin against the majority of the tested pathogens, worth to be further investigated.

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出版当年[2017]版:
大类 | 4 区 环境科学与生态学
小类 | 4 区 生化与分子生物学 4 区 化学综合
最新[2025]版:
大类 | 3 区 化学
小类 | 3 区 化学:综合 4 区 生化与分子生物学
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出版当年[2016]版:
Q3 CHEMISTRY, MULTIDISCIPLINARY Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
最新[2023]版:
Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Q3 CHEMISTRY, MULTIDISCIPLINARY

影响因子: 最新[2023版] 最新五年平均 出版当年[2016版] 出版当年五年平均 出版前一年[2015版] 出版后一年[2017版]

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第一作者机构: [a]Xuanwu Hospital, Capital Medical University, Beijing 100053, P. R. China
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