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Bioorg Med Chem ; 16(16): 7622-30, 2008 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-18657978

RESUMO

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.


Assuntos
Benzimidazóis/síntese química , Benzimidazóis/farmacologia , Tripanossomicidas/síntese química , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Animais , Benzimidazóis/química , Eletroquímica , Cinética , Espectrofotometria Ultravioleta , Tripanossomicidas/química
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