Design, synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl)fluoroquinolone derivatives |
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Authors: | Chai Yun Wang Jian Liu Mingliang Yi Hong Sun Lanying You Xuefu Guo Huiyuan |
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Institution: | a Institute of Medical Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China b The No.2 Hospital of Harbin, Harbin 150056, China |
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Abstract: | We report herein the design and synthesis of novel 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl) fluoroquinolone derivatives. The antibacterial activity of the newly synthesized compounds was evaluated and compared with gemifloxacin, levofloxacin and ciprofloxacin. Results reveal that compounds 10, 16, and 17 have good activity against all of the tested Gram-positive organisms including drug-resistance strains (MICs: 0.125-4 μg/mL). In addition, compounds 16 and 17 (MICs: 4 μg/mL) were 2- to 8-fold more potent than the reference drugs against Pseudomonas aeruginosa. |
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Keywords: | Fluoroquinolone Synthesis Antibacterial activity |
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