title: 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.
authors.affiliation: Departamento de Bioquímica e Immunologia, Faculdade de Medicina de Ribeirão, Universidade de São Paulo, Avenida Bandeirantes, 3900, CEP 14015-049, Ribeirão Preto, SP, Brazil.
authors.forename: A O
authors.initials: AO
authors.lastname: de Souza
authors.forename: F P
authors.initials: FP
authors.lastname: Hemerly
authors.forename: L
authors.initials: L
authors.lastname: Gomes-Cardoso
authors.forename: R M
authors.initials: RM
authors.lastname: Santa-Rita
authors.forename: L L
authors.initials: LL
authors.lastname: Leon
authors.forename: S L
authors.initials: SL
authors.lastname: de Castro
authors.forename: N
authors.initials: N
authors.lastname: Durán
mesh_terms: D000818:Animals; D007891:Leishmania / Q000187:drug effects*; D007896:Leishmaniasis / Q000188:drug therapy*; D021261:Parasitic Sensitivity Tests; D011437:Propylamines / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
chemical_list: D011437:Propylamines