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Synthesis, albumin interaction and anti Trypanosoma cruzi activity of copper (II) complex of norfloxacin and N-donor mixed ligand

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Document pages: 11 pages

Abstract: The first generation quinolone antibacterial agent norfloxacin copper (II) complex containing nitrogen donor heterocyclic ligand 2,2 - bipyridine (bipy) or 1,10-phenanthroline (phen) was prepared and characterized by IR, EPR, molar conductivity and elemental analysis. The experimental data showed that norfloxacin coordinated with copper (II) through carboxyl oxygen atom and ketone oxygen atom. The interaction of copper (II) complex with bovine serum albumin (BSA) and human serum albumin (HSA) was studied by tryptophan residue fluorescence quenching and copper (II) EPR spectroscopy. The results of fluorescence titration showed that the copper (II) complex had medium ability to quench the intrinsic fluorescence of protein by static quenchingmechanism. EPR experiments showed that BSA and HSA Cu(II) sites compete with NOR for Cu(II)-bipy and Cu(II)-phen to form protein mixed-ligand complexes. Copper(II) complexes, together with the corresponding ligands, were evaluated for their trypanocidal activity in vitro against Trypanosoma cruzi, the causative agent of Chagas disease. The tests performed using bloodstream trypomastigotes showed that the Cu(II)-N-donor precursors and the metal complexes were more active than the free fluoroquinolone.

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