2-propen-1-amine derivatives and their synthetic intermediates: activity against pathogenic trypanosomatids.
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.
de Souza
A O
AO
Departamento de Bioquímica e Immunologia, Faculdade de Medicina de Ribeirão, Universidade de São Paulo, Avenida Bandeirantes, 3900, CEP 14015-049, Ribeirão Preto, SP, Brazil.
Hemerly
F P
FP
Gomes-Cardoso
L
L
Santa-Rita
R M
RM
Leon
L L
LL
de Castro
S L
SL
Durán
N
N
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*
D011437:Propylamines