Design, synthesis, molecular docking, anti-Proteus mirabilis and urease inhibition of new fluoroquinolone carboxylic acid derivatives

作者：Abdullah Mohammed A A; Abuo Rahma Gamal El Din A A^*; Abdelhafez El Shimaa M N; Hassan Heba A; Abd El Baky Rehab M

来源：Bioorganic Chemistry, 2017, 70: 1-11.

DOI：10.1016/j.bioorg.2016.11.002

• Fluoroquinolones
• Hydroxamic acid
• Urease inhibitors
• Antibacterial
• Docking

New hydroxamic acid, hydrazide and amide derivatives of ciprofloxacin in addition to their analogues of levofloxacin were prepared and identified by different spectroscopic techniques. Some of the prepared compounds revealed good activity against the urease splitting bacteria, Proteus mirabilis. The urease inhibitory activity was investigated using indophenol method. Most of the tested compounds showed better activity than the reference acetohydroxamic acid (AHA). The ciprofloxacin hydrazide derivative 3a and levofloxacin hydroxamic acid 7 experienced the highest activity (IC50 = 1.22 mu M and 2.20 mu M, respectively). Molecular docking study revealed high spontaneous binding ability of the tested compounds to the active site of urease.

• 出版日期2017-2