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Type: Artigo de periódico
Title: 2-propen-1-amine derivatives and their synthetic intermediates: Activity against pathogenic trypanosomatids
Author: De Souza, AO
Hemerly, FP
Gomes-Cardoso, L
Santa-Rita, RM
Leon, LL
De Castro, SL
Duran, N
Abstract: The potential activity of three new derivatives of 3-(4'-Y-[1,1'-biphenyl]-4-yl)-3-(4-X-phenyl)-N,N-dimethyl-2-propen-1-amine (2-PAMs) was assayed against trypanosoma cruzi and Leishmania amazonensis. They showed higher activity against trypomastigotes and epimastigotes of T. cruzi than the standard drugs, crystal violet and nifurtimox. Besides these derivatives, a series of eleven 2-PAMs derivatives and the corresponding intermediates, biphenyl methanones (BPMs) were assayed against promastigotes of L. amazonensis, showing that the 2-PAMs were remarkably more active than the BPMs. The PAMs 2c, 2e and 2j were about 2-fold more active that pentamidine isothionate and between 27.2- and 46.4-fold less toxic to V79 mammalian cells. The present results encourage further studies, especially against intracellular parasites and in experimental animals.
Subject: 2-propen-1-amines
biphenyl methanones
biological activity
Trypanosoma cruzi
Leishmania amazonensis
Country: Itália
Editor: E I F T Srl
Rights: fechado
Date Issue: 2004
Appears in Collections:Artigos e Materiais de Revistas Científicas - Unicamp

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