Esr and spin trapping studies of two new potential ntitrypanosomal drugs

• Claudio Olea-Azar ^[1] ; Carolina Rigol ^[1] ; Lucía Opazo ^[1] ; Antonio Morello ^[1] ; Juan Diego Maya ^[1] ; Yolanda Repetto ^[1] ; Gabriela Aguirre ^[2] ; Hugo Cerecetto ^[2] ; Rossanna Di Maio ^[2] ; Mercedes González ^[2] ; Williams Porca ^[2]
  1. [1] Universidad de Chile

     Universidad de Chile

     Santiago, Chile

     
  2. [2] Universidad de la República

     Universidad de la República

     Uruguay

     
• Localización: Journal of the Chilean Chemical Society (Boletín de la Sociedad Chilena de Química), ISSN-e 0717-6309, ISSN 0366-1644, Vol. 48, Nº. 4, 2003, págs. 77-79
• Idioma: inglés
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• Resumen

  • The Electron Spin Resonance (ESR) spectra of radicals obtained from two new potential antitrypanosomal drugs by Trypanosoma cruzi reduction were analyzed. DMPO Spin Trapping was used to investigate the possible formation of free radicals in the trypanosome microsomal system. The Nitro 2 (4-(n-butyl)-1-(5-nitrofurfurylidene)semicarbazide) analogue of Nifurtimox showed better antiparasitic activity than N-oxide 1 (4-(n-butyl)-1-[(7-bromo-N1-oxidebenzo[1,2-c]1,2,5-oxadiazole-5-yl)methylidene]semicarbazide). Only Nitro 2 could produce oxygen redox cycling in T. cruzi epimastigotes. The ESR signal intensities were consistent with the trapping of hydroxyl radical. These results are in agreement with the biological observation that Nitro 2 showed antichagasic activity by an oxidative stress mechanism