Synthesis and antibacterial evaluation of novel 8-fluoro Norfloxacin derivatives as potential probes for methicillin and vancomycin-resistant Staphylococcus aureus

A series of novel 8-fluoro Norfloxacin derivatives and the hybrids of its piperazinyl derivatives incorporated with 1,3,5-triazine and pyrimidine were synthesized. All the above compounds were evaluated for their antibacterial activity against Klebsiella pneumoniae, methicillin-resistant Staphylococcus aureus and methicillin & vancomycin-resistant S. aureus. Among all, compounds having Morpholine, N-methyl/phenyl/benzyl/pyrimidinyl piperazines and n-butylamine substitution at C-7 position, have shown increased potency in comparison to norfloxacin and ciprofloxacin.

A series of novel 8-fluoro Norfloxacin derivatives and the hybrids of its piperazinyl derivatives were synthesized. Some of synthesized compounds have shown better activity then norfloxacin and ciprofloxacin.Figure optionsDownload as PowerPoint slideResearch highlights
► The design and synthesis of new hybrid with multiple targets is a successful approach to conquer the problem of resistance.
► A series of novel 8-fluoro Norfloxacin derivatives and the hybrids of its piperazinyl derivatives incorporated with 1,3,5-triazine and pyrimidine have been synthesized.
► All the above compounds have been evaluated for their antibacterial activity against Klebsiella pneumoniae, methicillin-resistant Staphylococcus aureus and methicillin and vancomycin-resistant Staphylococcus aureus.
► Among all the compounds having Morpholine, N-methyl/phenyl/benzyl/pyrimidinyl piperazines and n-butyl amine substitution at C-7 position have shown promising activity approximately 35 fold greater than Norfloxacin.