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  • 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, Durán N.
    Journal: J Chemother; 2004 Dec; 16(6):530-3. PubMed ID: 15700843.
    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.
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