title: Nitrofurylsemicarbazone rhenium and ruthenium complexes as anti-trypanosomal agents.
abstract: Rhenium and ruthenium complexes of the type [Re(V)OCl(2)(PPh(3))L] and [Ru(II)Cl(2)(DMSO)(2)L], where L are 5-nitrofurylsemicarbazone derivatives, were prepared in an effort to obtain new anti-trypanosomal agents combining the recognized biological activity of these metals and the trypanocidal activity of the free ligands. Rhenium complexes resulted unstable in aqueous solution not allowing their use as potential drugs. On the other hand, complexation to ruthenium of the bioactive ligands lead to the lack of antiprotozoa activity even though free radical production and redox cycling induction were detected when the compounds were incubated in presence of Trypanosoma cruzi cells. The lack of anti-trypanosomal activity of ruthenium complexes could be explained on the basis of their high protein binding capacity and their high hydrophilicity.
authors.affiliation: Cátedra de Química Inorgánica, DEC, Facultad de Química, Universidad de la República, Montevideo, Uruguay.
authors.forename: Lucía
authors.initials: L
authors.lastname: Otero
authors.forename: Gabriela
authors.initials: G
authors.lastname: Aguirre
authors.forename: Lucía
authors.initials: L
authors.lastname: Boiani
authors.forename: Ana
authors.initials: A
authors.lastname: Denicola
authors.forename: Carolina
authors.initials: C
authors.lastname: Rigol
authors.forename: Claudio
authors.initials: C
authors.lastname: Olea-Azar
authors.forename: Juan Diego
authors.initials: JD
authors.lastname: Maya
authors.forename: Antonio
authors.initials: A
authors.lastname: Morello
authors.forename: Mercedes
authors.initials: M
authors.lastname: González
authors.forename: Dinorah
authors.initials: D
authors.lastname: Gambino
authors.forename: Hugo
authors.initials: H
authors.lastname: Cerecetto
mesh_terms: D000818:Animals; D004563:Electrochemistry; D004578:Electron Spin Resonance Spectroscopy; D009682:Magnetic Resonance Spectroscopy; D009581:Nitrofurans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012211:Rhenium / Q000737:chemistry*; D012428:Ruthenium / Q000737:chemistry*; D012664:Semicarbazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013055:Spectrophotometry, Infrared; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D009581:Nitrofurans; D009942:Organometallic Compounds; D012664:Semicarbazones; D014344:Trypanocidal Agents; D012211:Rhenium; D012428:Ruthenium