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Determination and characterization of new benzimidazoles with activity against Trypanosoma cruzi by UV spectroscopy and HPLC

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2008-08-15
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Brain Isasi, S.
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Determination and characterization of new benzimidazoles with activity against Trypanosoma cruzi by UV spectroscopy and HPLC
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Author
  • Brain Isasi, S.;
  • Quezada Aburto, Cristián Salvador;
  • Pessoa Mahana, Hernán;
  • Morello Casté, Antonio;
  • Kogan Bocian, Marcelo;
  • Álvarez Lueje, Alejandro;
Abstract
This work presents the development of analytical methodologies by UV spectrophotometry and HPLC to characterize five nitroarylbenzimidazole derivatives with activity against Trypanosoma cruzi: NB, BNB, PNB, PMNB and PCNB. Both methodologies exhibit adequate repeatabilities and reproducibilities (CV < 2%) and recoveries higher than 98%. The ionization constants (pK(a)), lipophilicity (log P) and effective permeability (Pe) are reported. The five compounds present an inhibitory effect on the T. cruzi growth (epimastigotes) at 1-100 mu M concentration range in an order rank of PMNB > PCNB > PNB > BNB > NB. Additionally, cyclic voltammetric data reveal that the nitroarylbenzimidazole derivatives might sustain their effects on growth and oxygen uptake on T. cruzi epimastigotes.
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URI: https://repositorio.uchile.cl/handle/2250/120521
ISSN: 0968-0896
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BIOORGANIC & MEDICINAL CHEMISTRY 16(16):7622-7630
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