Synthesis and biological evaluation of a mutual prodrug of norfloxacin and fenbufen

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Abstract

Objectives The study aimed to synthesize a mutual prodrug of norfloxacin and fenbufen with an objective of obtaining an effective and safer anti-inflammatory drug with useful antimicrobial actions. Methods An amide-based mutual prodrug (NF-FN) was prepared following a single-step synthesis by condensing norfloxacin with fenbufen under appropriate laboratory conditions. Its structure was established on the basis of IR, NMR, Mass spectral data and elemental analysis. The prodrug (NF-FN) was evaluated for in-vitro antibacterial activity against two gram positive (Staphylococcus aureus & Bacillus subtilis) and two gram negative bacterial strains (Escherichia coli & Klebsiella pneumonia). The in-vivo anti-inflammatory activity and ulcerogenicity of the synthesized prodrug were investigated in Wistar albino rats at the doses of 10 and 30 mg/kg body weight, respectively. Results The synthesized prodrug (NF-FN) showed very good activity against S. aureus & E. coli with MIC-6.25 μg/mL, and good activity against B. subtilis & K. pneumonia with MIC-12.5 μg/mL. Its anti-inflammatory activity was found to be better than that of the parent drug fenbufen. It was also observed to less severe on gastric mucosa in comparison to reference drug, fenbufen. Conclusion The prodrug showed promising results as anti-inflammatory agent however, its antibacterial action was found to be slightly weaker than the other parent drug norfloxacin.

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Husain, A., Ahmad, A., & Khan, S. A. (2016). Synthesis and biological evaluation of a mutual prodrug of norfloxacin and fenbufen. Journal of Taibah University Medical Sciences, 11(3), 277–281. https://doi.org/10.1016/j.jtumed.2016.03.003

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