A group of N4-piperazinyl derivatives of norfloxacin 1  was synthesized and characterized by different spectroscopic techniques. The N4-piperazinyl substituents in the new compounds 2  , 3a-c,  4a-d  and 5a-e were designed to alter the electronic, steric and physicochemical properties of norfloxacin structure.The antibacterial properties of the newly synthesized compounds were evaluated against Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae and Staphylococcus aureus strains using norfloxacin as a reference. Most of the tested compounds exhibited improved activity against E. coli and K. pneumoniae if compared to norfloxacin and five of them were more active against P. aeruginosa. None of the new compounds was more active against S. aureusthan norfloxacin. The minimum inhibitory concentrations of the new compounds were shown to be correlated with lipophilicity, polarizability and topology parameters of the tested compounds.

New <i>N-4</i> piperazinyl derivatives of norfloxacin: Correlation of lipophilicity, polarizability and topology parameters with antibacterial activity

247th National Meeting (2014)

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New N-4 piperazinyl derivatives of norfloxacin: Correlation of lipophilicity, polarizability and topology parameters with antibacterial activity