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

作者：Chai, Yun; Wang, Jian; Liu, Mingliang^*; Yi, Hong; Sun, Lanying; You, Xuefu; Guo, Huiyuan

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(11): 3377-3380.

DOI：10.1016/j.bmcl.2011.04.002

• Fluoroquinolone
• Synthesis
• Antibacterial activity

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.

• 出版日期2011-6-1
• 单位中国医学科学院医药生物技术研究所