Insight into the bioreductive mode of action of antitrypanosomal 5-nitrofuryl containing thiosemicarbazones.
In order to get insight into the trypanocidal mechanism of action of a series of 5-nitrofuryl containing thiosemicarbazones some studies related to their bioreduction were performed. Electron spin resonance spectra of radicals generated in T. cruzi by compounds' bioreduction were analyzed. Three different patterns of ESR signals were observed for the different assayed compounds. These results were in agreement with the changes in the T. cruzi-oxygen uptake promoted by these compounds. On the other hand, free-radical scavenger properties, measured as oxygen radical absorbance capacity (ORAC), did not seem to correlate with the trypanocidal activity.
Otero
L
L
Cátedra de Química Inorgánica, DEC, Facultad de Química, Universidad de la República, Gral. Flores 2124, 11200 Montevideo, Uruguay.
Maya
J D
JD
Morello
A
A
Rigol
C
C
Barriga
G
G
Rodríguez
J
J
Folch
C
C
Norambuena
E
E
González
M
M
Azar
C Olea
CO
Cerecetto
H
H
Gambino
D
D
D000818:Animals; D004578:Electron Spin Resonance Spectroscopy; D016166:Free Radical Scavengers / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D009581:Nitrofurans / Q000737:chemistry*; D010084:Oxidation-Reduction / Q000187:drug effects; D010101:Oxygen Consumption / Q000187:drug effects; D017382:Reactive Oxygen Species / Q000378:metabolism; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects / Q000378:metabolism
D016166:Free Radical Scavengers; D009581:Nitrofurans; D017382:Reactive Oxygen Species; D013882:Thiosemicarbazones; D014344:Trypanocidal Agents