Synthesis and antibacterial activity of novel fluoroquinolone analogs

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Abstract

Fluoroquinolone analogs were synthesized by reductive amination and screened for their antibacterial activities against E. coli K12 and S. aureus RN4220. Out of 18 compounds under the present study, 8 compounds were found most active against S. aureus RN4220 and E. coli K12, respectively, with MIC < 0.062 μg/mL, which sufficiently potent for possible clinical application. All synthesized compounds were characterized by various spectroscopic techniques viz. IR, 1 H and 13 C NMR, and mass spectrometry. Out of these, one compound (3) was also characterized by the single crystal X-ray analysis. In order to understand the molecular interactions of these compounds (5-22) with enzyme DNA gyrase, molecular docking of two compounds viz. compounds 9 and 11 was also performed and we found promising results.

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Dixit, S. K., Yadav, N., Kumar, S., Good, L., & Awasthi, S. K. (2014). Synthesis and antibacterial activity of novel fluoroquinolone analogs. Medicinal Chemistry Research, 23(12), 5237–5249. https://doi.org/10.1007/s00044-014-1049-2

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