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Abstract

SYNTHESIS, CHARACTERIZATION AND ANTI-INFLAMMATORY ACTIVITY OF SPARFLOXACIN METAL COMPLEX

Sakshi D. Ambhore*, Puja M. Bhujang, Pooja C. Mane, Urmila S. Sule and Swati B. Thoke

ABSTRACT

The fluoroquinolones are synthetic antibiotics, active against aerobic Gram (-ve) and Gram (+ve) microorganisms. Fluoroquinolones possess 3-carboxylate group and 4-keto group which are essential for formation of metal complex. The lipophilicity of the drug is increased through the formation of chelate and drug action is significantly increased due to effective permeability of the drug into the site of action. The activity of biometals is attained through the formation of complexes with different bioligands and the mode of biological action for complexes depends upon the thermodynamic and kinetic properties. Interaction of various metal ions with antibiotics may enhance their antimicrobial activity as compared to that of free ligands. Fe (III) complexes of sparfloxacin in presence of neutral bidentate ligand (N-N) donors 1, 10-Phenanthroline have been synthesized. Fe (III) complexes of sparfloxacin complexes were confirmed by
physiochemical parameters and spectroscopic data (Quantitative UV, Mass Spectrometry, FT-IR spectroscopy and NMR spectroscopy). The stability study of all novel complexes were evaluated as per ICH guidelines and all the complexes were found to be stable. Sparfloxacin complexes were evaluated for their antibacterial activity against two different microorganisms (Escherichia coli and Staphylococcus aureus).

Keywords: Metal complex, Metalloantibiotics, Fluoroquinolones, Sparfloxacin, DNA- interaction.


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