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Type: Artigo de periódico
Title: In vitro trypanocidal activities of a novel series of N,N-dimethyl-2-propen-1-amine derivative
Author: DeConti, R
Rita, RMS
deSouza, EM
Melo, PS
Haun, M
DeCastro, SL
Duran, N
Abstract: The trypanocidal activity of several 3-(4'-bromo-[1,1'-biphenyl]-4-yl)-3-(4-X-phenyl)-N,N-dimethyl-2-propen-1-amine derivatives on the three evolutionary stages of Trypanosoma cruzi, namely the bloodstream trypomastigote form and both the proliferative epimastigote and amastigote forms, were studied. For both proliferative forms of T. cruzi, total lysis occurred at 10-60 mu M and for trypomastigotes at 40-200 mu M. The following order of susceptibility was established: amastigotes > epimastigotes > trypomastigotes. The most were the bromo (X = g) and unsubstituted (X = b) compounds, which had 13- and 8-fold higher activity against trypomastigotes, respectively, than nifurtimox. Cytotoxicity in the Chinese hamster V-79 cell line, measured as inhibition of cell proliferation showed that all the compounds had the same range of IC50 (7.0-12.4 mu M). The halogen (X = a,g,h) and the unsubstituted derivatives (X = b) were the least toxic in the series together with the compound (X = f).
Subject: Chagas's disease
Trypanosoma cruzi
synthetic drugs
Country: Inglaterra
Editor: Faculty Press
Rights: fechado
Date Issue: 1996
Appears in Collections:Artigos e Materiais de Revistas Científicas - Unicamp

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