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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Insight into the Bioreductive Mode of Action of Antitrypanosomal 5- Nitrofuryl Containing Thiosemicarbazones

Author(s): D. Gambino, L. Otero, J. D. Maya, A. Morello, C. Rigol, G. Barriga, J. Rodriguez, C. Folch, E. Norambuena, M. Gonzalez, C. Olea Azar and H. Cerecetto

Volume 4, Issue 1, 2008

Page: [11 - 17] Pages: 7

DOI: 10.2174/157340608783331470

Price: $65

Abstract

In order to get insight into the trypanocidal mechanism of action of a series of 5-nitrofuryl containing hiosemicarbazones 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.

Keywords: Chagas disease, 5-nitrofuryl containing thiosemicarbazones, ORAC, ESR


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