Synthesis, antimycobacterial and antibacterial activity of ciprofloxacin derivatives containing a N-substituted benzyl moiety

We report herein a series of novel ciprofloxacin (CPFX) derivatives. Results reveal that compound 4f has good in vitro activity against all of the tested Gram-positive strains including MRSA and MRSE (MICs: 0.06-32 μg/mL) which is two to eight-fold more potent than or comparable to the parent drug CPFX (MICs: 0.25-128 μg/mL), Gram-negative bacteria P. aeruginosa (MICs: 0.5-4 μg/mL) and mycobacterium tuberculosis H37Rv ATCC 27294 (MIC: 1 μg/mL).