title: Copper(II) complexes with sparfloxacin and nitrogen-donor heterocyclic ligands: Structure-activity relationship.
abstract: Three novel neutral mononuclear copper(II) complexes of the third-generation quinolone antibacterial drug sparfloxacin in the presence of a nitrogen donor heterocyclic ligand 2,2'-bipyridine, 1,10-phenanthroline or 2,2'-dipyridylamine have been prepared and characterized physicochemically and spectroscopically. The resultant complexes are of the type Cu(sparfloxacinato)(N-donor)Cl. Copper(II) is pentacoordinate having a distorted square pyramidal geometry. Molecular modeling calculations have been performed in order to propose the lowest energy model structure of the complexes. The interaction of the complexes with calf-thymus DNA has been investigated with diverse spectroscopic techniques and has shown that the complexes can bind to calf-thymus DNA by the intercalative mode. The antimicrobial activity of the complexes has been tested on three different microorganisms. The Cu(sparfloxacinato)(N-donor)Cl complexes are among the most active ones against Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus, when compared to the other corresponding copper-quinolone complexes studied by our group and their antimicrobial activity is increased in the order bipyam<bipy=phen. We have also shown that two of the Cu(sparfloxacinato)(N-donor)Cl complexes have decreased the viability of human leukemia cells HL-60 in a time-dependent manner.
authors.affiliation: Institute of Physical Chemistry, NCSR Demokritos, GR-15310 Aghia Paraskevi Attikis, Greece.
authors.forename: Eleni K
authors.initials: EK
authors.lastname: Efthimiadou
authors.forename: Maria E
authors.initials: ME
authors.lastname: Katsarou
authors.forename: Alexandra
authors.initials: A
authors.lastname: Karaliota
authors.forename: George
authors.initials: G
authors.lastname: Psomas
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D003300:Copper / Q000737:chemistry*; D024841:Fluoroquinolones / Q000737:chemistry* / Q000494:pharmacology; D018922:HL-60 Cells; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D008826:Microbial Sensitivity Tests; D009584:Nitrogen / Q000737:chemistry*; D013057:Spectrum Analysis; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D006571:Heterocyclic Compounds; D008024:Ligands; D003300:Copper; D009584:Nitrogen; C061363:sparfloxacin