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Novel N-4-Piperazinyl Ciprofloxacin-Ester Hybrids: Synthesis, Biological Evaluation, and Molecular Docking Studies

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Abstract

A series of novel N-4-piperazinyl ciprofloxacin-ester hybrids has been synthesized and the structures confirmed by1H and 13C NMR, FT-IR spectral data, and elemental analysis. The products have been tested in vitro for their antibacterial activity against six bacterial strains (MRSA, Staphylococcus epidermidis, Bacillus subtilis, Escherichia coli,Salmonella enterica, and Klebsiella pneumoniae) and have demonstrated good antibacterial activity with MIC values range 6.25–200 µg/mL. Antifungal and cytotoxic activities of the products have been tested against Candida kefyr and human leukemia K562 cell line, respectively. All compounds inhibit growth of K562 cells more efficiently than the parent ciprofoxacin in a dose- and duration-dependent way. Molecular docking studies performed for the compound 3i indicates that similarly to ciprofloxacin it can act as an inhibitor of S. aureus DNA gyrase.

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ACKNOWLEDGMENTS

We gratefully acknowledge financial support from the Research Council of the University of Tabriz.

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Correspondence to H. Mostafavi.

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Shahbazi, A., Mostafavi, H., Zarrini, G. et al. Novel N-4-Piperazinyl Ciprofloxacin-Ester Hybrids: Synthesis, Biological Evaluation, and Molecular Docking Studies. Russ J Gen Chem 90, 1558–1565 (2020). https://doi.org/10.1134/S1070363220080265

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