Effect of ruthenium complexation on trypanocidal activity of 5-nitrofuryl containing thiosemicarbazones.
In the search of new therapeutic tools for the treatment of American Trypanosomiasis, the largest parasitic disease burden in the American continent, three series of novel ruthenium complexes of the formula [RuCl(2)(HL)(2)], [RuCl(3)(dmso)(HL)] and [RuCl(PPh(3))(L)(2)] with bioactive 5-nitrofuryl containing thiosemicarbazones as ligands (HL neutral, L monoanionic) were synthesized and characterized. Their in vitro growth inhibition activity against Trypanosoma cruzi and the effect of co-ligands in related physicochemical properties i.e. nitro moiety redox potential, lipophilicity and free radical scavenger capacity were evaluated. Results show that although a loss of activity was observed as a consequence of ruthenium complexation, lipophilicity and free radical scavenger capacity of the obtained complexes could be correlated to their trypanocidal effect.
Facultad de Química, Universidad de la República, Gral. Flores 2124, C.C. 1157, Montevideo 11800, Uruguay.
Mariana
M
Pagano
Bruno
B
Demoro
Jeanette
J
Toloza
Lucía
L
Boiani
Mercedes
M
González
Hugo
H
Cerecetto
Claudio
C
Olea-Azar
Ester
E
Norambuena
Dinorah
D
Gambino
Lucía
L
Otero
D008024:Ligands; D015394:Molecular Structure; D009581:Nitrofurans / Q000737:chemistry* / Q000494:pharmacology; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D012428:Ruthenium / Q000737:chemistry / Q000494:pharmacology; D013882:Thiosemicarbazones / Q000737:chemistry* / Q000494:pharmacology; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects
D008024:Ligands; D009581:Nitrofurans; D009942:Organometallic Compounds; D013882:Thiosemicarbazones; D014344:Trypanocidal Agents; D012428:Ruthenium