Nitrofurylsemicarbazone rhenium and ruthenium complexes as anti-trypanosomal agents.
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.
Otero
Lucía
L
Cátedra de Química Inorgánica, DEC, Facultad de Química, Universidad de la República, Montevideo, Uruguay.
Aguirre
Gabriela
G
Boiani
Lucía
L
Denicola
Ana
A
Rigol
Carolina
C
Olea-Azar
Claudio
C
Maya
Juan Diego
JD
Morello
Antonio
A
González
Mercedes
M
Gambino
Dinorah
D
Cerecetto
Hugo
H
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
D009581:Nitrofurans; D009942:Organometallic Compounds; D012664:Semicarbazones; D014344:Trypanocidal Agents; D012211:Rhenium; D012428:Ruthenium