Literature DB >> 18657978

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

Stephanie Brain-Isasi1, Cristián Quezada, Hernán Pessoa, Antonio Morello, Marcelo J Kogan, Alejandro Alvarez-Lueje.   

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 microM 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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Year:  2008        PMID: 18657978     DOI: 10.1016/j.bmc.2008.07.021

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  1 in total

1.  Evaluation of the membrane permeability (PAMPA and skin) of benzimidazoles with potential cannabinoid activity and their relation with the Biopharmaceutics Classification System (BCS).

Authors:  M Javiera Alvarez-Figueroa; C David Pessoa-Mahana; M Elisa Palavecino-González; Jaime Mella-Raipán; Cristián Espinosa-Bustos; Manuel E Lagos-Muñoz
Journal:  AAPS PharmSciTech       Date:  2011-05-04       Impact factor: 3.246

  1 in total

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