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<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.
Brain-Isasi
Stephanie
S
Chemical and Pharmaceutical Sciences Faculty, University of Chile. P.O. Box 233, Santiago 1, Chile.
Quezada
Cristián
C
Pessoa
Hernán
H
Morello
Antonio
A
Kogan
Marcelo J
MJ
Alvarez-Lueje
Alejandro
A
D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004563:Electrochemistry; D007700:Kinetics; D013056:Spectrophotometry, Ultraviolet; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
D001562:Benzimidazoles; D014344:Trypanocidal Agents