title: Ligational behaviour of lomefloxacin drug towards Cr(III), Mn(II), Fe(III), Co(II), Ni(II), Cu(II), Zn(II), Th(IV) and UO(2)(VI) ions: synthesis, structural characterization and biological activity studies.
abstract: Nine new mononuclear Cr(III), Mn(II), Fe(III), Co(II), Ni(II), Cu(II), Zn(II), Th(IV) and UO(2)(VI) complexes of lomefloxacin drug were synthesized. The structures of these complexes were elucidated by elemental analyses, IR, XRD, UV-vis, (1)H NMR as well as conductivity and magnetic susceptibility measurements and thermal analyses. The dissociation constants of lomefloxacin and stability constants of its binary complexes have been determined spectrophotometrically in aqueous solution at 25±1°C and at 0.1 M KNO(3) ionic strength. The discussion of the outcome data of the prepared complexes indicate that the lomefloxacin ligand behaves as a neutral bidentate ligand through OO coordination sites and coordinated to the metal ions via the carbonyl oxygen and protonated carboxylic oxygen with 1:1 (metal:ligand) stoichiometry for all complexes. The molar conductance measurements proved that the complexes are electrolytes. The powder XRD study reflects the crystalline nature for the investigated ligand and its complexes except Mn(II), Zn(II) and UO(2)(II). The geometrical structures of these complexes are found to be octahedral. The thermal behaviour of these chelates is studied where the hydrated complexes lose water molecules of hydration in the first steps followed by decomposition of the anions, coordinated water and ligand molecules in the subsequent steps. The activation thermodynamic parameters are calculated using Coats-Redfern and Horowitz-Metzger methods. A comparative study of the inhibition zones of the ligand and its metal complexes indicates that metal complexes exhibit higher antibacterial effect against one or more bacterial species than the free LFX ligand. The antifungal and anticancer activities were also tested. The antifungal effect of almost metal complexes is higher than the free ligand. LFX, [Co(LFX)(H(2)O)(4)]·Cl(2) and [Zn(LFX)(H(2)O)(4)]·Cl(2) were found to be very active with IC50 values 14, 11.2 and 43.1, respectively. While, other complexes had been found to be inactive at lower concentration than 100 μg/ml.
authors.affiliation: Pharmaceutical Chemistry Department, Faculty of Pharmacy, Misr International University, Cairo, Egypt.
authors.forename: Hanan F
authors.initials: HF
authors.lastname: Abd el-Halim
authors.forename: Gehad G
authors.initials: GG
authors.lastname: Mohamed
authors.forename: Maher M I
authors.initials: MM
authors.lastname: el-Dessouky
authors.forename: Walaa H
authors.initials: WH
authors.lastname: Mahmoud
mesh_terms: D045744:Cell Line, Tumor; D002857:Chromium / Q000737:chemistry; D003035:Cobalt / Q000737:chemistry; D003300:Copper / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D007477:Ions; D007501:Iron / Q000737:chemistry; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008345:Manganese / Q000737:chemistry; D008956:Models, Chemical; D009532:Nickel / Q000737:chemistry; D010100:Oxygen / Q000737:chemistry; D013696:Temperature; D013818:Thermogravimetry / Q000379:methods; D013910:Thorium / Q000737:chemistry; D015032:Zinc / Q000737:chemistry
chemical_list: D024841:Fluoroquinolones; D007477:Ions; D008024:Ligands; D002857:Chromium; D003035:Cobalt; D008345:Manganese; D013910:Thorium; D003300:Copper; D009532:Nickel; D007501:Iron; D015032:Zinc; C053091:lomefloxacin; D010100:Oxygen