2-Propen-1-amine Derivatives and Their Synthetic Intermediates: Activity Against Pathogenic Trypanosomatids

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.

Keywords:

• 2-Propen-1-amines
• biphenyl methanones
• biological activity
• Trypanosoma cruzi
• Leishmania amazonensis