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Design, synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl) fluoroquinolone derivatives

  作者 Chai, Y; Wang, J; Liu, ML; Yi, H; Sun, LY; You, XF; Guo, HY  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2011年21-11;  页码  3377-3380  
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[摘要]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 mu g/mL). In addition, compounds 16 and 17 (MICs: 4 mu g/mL) were 2- to 8-fold more potent than the reference drugs against Pseudomonas aeruginosa. (C) 2011 Elsevier Ltd. All rights reserved.

 
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