Phenoxyacetohydrazones against Trypanosoma cruzi

Herein, we reported the design, synthesis, antitrypanosomal and cytotoxic evaluation of a new phenoxyacetohydrazones series. All derivatives were assayed against bloodstream trypomastigote forms T. cruzi (Y strain) intracellular amastigotes using model L-929 cells infected with trypomastigotes Tulahuen strain. Compound (E)-N′-(3.4-dihydroxybenzylidene)-2-phenoxyacetohydrazide (11) showed activity (IC50/24 h = 10.3 µM) equivalent to that benznidazole selectivity index (SI) 46. Against cultures, (E)-N′-((5-nitrofuran-2-yl) methylene)-2-phenoxyacetohydrazide (19) was active at nanomolar range (IC50/96 40 nM), being about 38-fold more than standard drug SI equal 2500. Thus, 11 19 could be considered good prototypes for development candidates Chagas disease therapy.