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

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...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2008-08, Vol.16 (16), p.7622-7630
Hauptverfasser: Brain-Isasi, Stephanie, Quezada, Cristián, Pessoa, Hernán, Morello, Antonio, Kogan, Marcelo J., Álvarez-Lueje, Alejandro
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Sprache:eng
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Zusammenfassung: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 (p K 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 μM 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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2008.07.021