RESUMO
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 grampositive [Staphylococcus aureusand Bacillus subtilis] and two gram negative bacterial strains [Escherichia coli and Klebsiella pneumonia]. The in-vivo antiinflammatory 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 and E. coli with MIC-6.25 mg/ mL, and good activity against B. subtilis and K. pneumonia with MIC-12.5 mg/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