title: Antibacterial, antifungal and in vitro antileukaemia activity of metal complexes with thiosemicarbazones.
abstract: 1-phenyl-3-methyl-4-benzoyl-5-pyrazolone 4-ethyl-thiosemicarbazone (HL) and its copper(II), vanadium(V) and nickel(II) complexes: [Cu(L)(Cl)]·C₂H₅OH·(1), [Cu(L)₂]·H₂O (2), [Cu(L)(Br)]·H₂O·CH₃OH (3), [Cu(L)(NO₃)]·2C₂H₅OH (4), [VO₂(L)]·2H₂O (5), [Ni(L)₂]·H₂O (6), were synthesized and characterized. The ligand has been characterized by elemental analyses, IR, (1) H NMR and (13) C NMR spectroscopy. The tridentate nature of the ligand is evident from the IR spectra. The copper(II), vanadium(V) and nickel(II) complexes have been characterized by different physico-chemical techniques such as molar conductivity, magnetic susceptibility measurements and electronic, infrared and electron paramagnetic resonance spectral studies. The structures of the ligand and its copper(II) (2, 4), and vanadium(V) (5) complexes have been determined by single-crystal X-ray diffraction. The composition of the coordination polyhedron of the central atom in 2, 4 and 5 is different. The tetrahedral coordination geometry of Cu was found in complex 2 while in complex 4, it is square planar, in complex 5 the coordination polyhedron of the central ion is distorted square pyramid. The in vitro antibacterial activity of the complexes against Escherichia coli, Salmonella abony, Staphylococcus aureus, Bacillus cereus and the antifungal activity against Candida albicans strains was higher for the metal complexes than for free ligand. The effect of the free ligand and its metal complexes on the proliferation of HL-60 cells was tested.
authors.affiliation: Inorganic Chemistry Department, Faculty of Pharmacy, University of Medicine and Pharmacy "Carol Davila", Bucharest, Romania.
authors.forename: Elena
authors.initials: E
authors.lastname: Pahontu
authors.forename: Felicia
authors.initials: F
authors.lastname: Julea
authors.forename: Tudor
authors.initials: T
authors.lastname: Rosu
authors.forename: Victor
authors.initials: V
authors.lastname: Purcarea
authors.forename: Yurie
authors.initials: Y
authors.lastname: Chumakov
authors.forename: Petru
authors.initials: P
authors.lastname: Petrenco
authors.forename: Aurelian
authors.initials: A
authors.lastname: Gulea
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology; D001409:Bacillus cereus / Q000187:drug effects / Q000254:growth & development; D002176:Candida albicans / Q000187:drug effects / Q000254:growth & development; D049109:Cell Proliferation / Q000187:drug effects; D056831:Coordination Complexes / Q000737:chemistry* / Q000494:pharmacology; D003300:Copper / Q000737:chemistry; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D004578:Electron Spin Resonance Spectroscopy; D004926:Escherichia coli / Q000187:drug effects / Q000254:growth & development; D018922:HL-60 Cells; D006801:Humans; D015473:Leukemia, Promyelocytic, Acute / Q000473:pathology; D009682:Magnetic Resonance Spectroscopy; D008670:Metals / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009532:Nickel / Q000737:chemistry; D012475:Salmonella / Q000187:drug effects / Q000254:growth & development; D013211:Staphylococcus aureus / Q000187:drug effects / Q000254:growth & development; D013882:Thiosemicarbazones / Q000737:chemistry*; D014639:Vanadium / Q000737:chemistry
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D056831:Coordination Complexes; D008670:Metals; D013882:Thiosemicarbazones; D014639:Vanadium; D003300:Copper; D009532:Nickel
keywords: Cu(II), V(V) and Ni(II) complexes; antimicrobial activity; antiproliferative activity; crystal structure; thiosemicarbazone