Abstract
We report herein the design and synthesis of a series of novel miconazole-based ciprofloxacin hybrids with remarkable antimicrobial activities by introducing antifungal fragments to the clinic drug ciprofloxacin. Bioactive assay manifested that 1-cyclopropyl-7-[4-[1-(2,4-difluorophenyl)-2-(1H-imidazol-1-yl)ethyl]piperazin-1-yl]-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid displayed good in vitro biological activities, which were comparable or even better than the reference drugs, miconazole and ciprofloxacin. Especially for Bacillus subtilis, the 1-cyclopropyl-7-[4-[1-(2,4-difluorophenyl)-2-(1H-imidazol-1-yl)ethyl]piperazin-1-yl]-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid(0.25 μg/cm3) was eightfold more potent than the parent drug ciprofloxacin (2 μg/cm3). Our prepared hybrids obviously have promises to be further developed as antimicrobial agents.
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Gu, XL., Liu, HB., Jia, QH. et al. Design and synthesis of novel miconazole-based ciprofloxacin hybrids as potential antimicrobial agents. Monatsh Chem 146, 713–720 (2015). https://doi.org/10.1007/s00706-014-1364-9
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DOI: https://doi.org/10.1007/s00706-014-1364-9