In vitro trypanocidal activities of a novel series of N, N-dimethyl-2-propen-1-amine derivative.
The trypanocidal activity of several 3-(4'-bromo-[1,1-biphenyl]-4-yl) -3-(4-X-phenyl)-N,N-dimethyl-2-propen-1-amine derivatives of the three evolutionary stages of Trypanosoma cruzi, namely the bloodstream trypomastigote form and both the proliferative epimastigote and amastigote forms, were studied. For both proliferative forms of T. cruzi, total lysis occurred at 10-60 microM for trypomastigotes at 40-200 muM. The following order of susceptibility was established: amastigotes > epimastigotes > trypomastigotes. The most were the bromo (X = g) and unsubstituted (X = b) compounds, which had 13- and 8-fold higher activity against trypomastigotes, respectively, than nifurtimox. Cytotoxicity in the Chinese hamster V-79 cell line, measured as inhibition of cell proliferation showed that all the compounds had the same range of IC50 (7.0-12.4 muM). The halogen (X = a,g,h) and the unsubstituted derivatives (X = b) were the least toxic in the series together with the compound (X = f).
De Conti
R
R
Instituto de Química, Universidade Estadual de Campinas, SP, Brazil.
Rita
R M
RM
de Souza
E M
EM
Melo
P S
PS
Haun
M
M
De Castro
S L
SL
Durán
N
N
D000818:Animals; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D004353:Drug Evaluation, Preclinical; D011437:Propylamines / Q000494:pharmacology* / Q000633:toxicity; D014344:Trypanocidal Agents / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
D011437:Propylamines; D014344:Trypanocidal Agents