Abstract
A series of 14 (E)-cinnamic N-acylhydrazone derivatives, designed through molecular hybridization between the (E)-1-(benzo[d][1,3]dioxol-5-yl)-3-(4-bromophenyl)prop-2-en-1-one and (E)-3-hydroxy-N'-((2-hydroxynaphthalen-1-yl)methylene)-7-methoxy-2-naphthohydrazide, were tested for in vitro antiparasitic activity upon axenic amastigote forms of Leishmania donovani and bloodstream forms of Trypamosoma brucei rhodesiense. The derivative (2E)-3-(4-hydroxy-3-methoxy-5-nitrophenyl)-N'-[(1E)-phenylmethylene]acrylohydrazide showed moderate antileishmanial activity (IC50 = 6.27 µM) when compared to miltefosine, the reference drug (IC50 = 0.348 µM). However, the elected compound showed an excellent selectivity index; in one case it was not cytotoxic against mammalian L-6 cells. The most active antitrypanosomal compound, the derivative (E)-N'-(3,4-dihydroxybenzylidene)cinnamohydrazide (IC50 = 1.93 µM), was cytotoxic against mammalian L-6 cells.
Highlights
IntroductionAfrican sleeping sickness and leishmaniasis continue to cause significant public health problems
African sleeping sickness and leishmaniasis continue to cause significant public health problems.These parasitic diseases are responsible for a high rate of mortality and morbidity each year in tropical and subtropical countries [1].African sleeping sickness is caused by the protozoan parasite Trypanosoma brucei exclusively in sub-Saharan Africa
They’re different kinetoplastid pathogens have a similar genomic organization and cellular structures [12]. This evolutionary resemblance and the previous results obtained by our research group with T. cruzi encouraged us to evaluate a series of fourteen of these derivatives upon axenic amastigote forms of Leishmania donovani and against bloodstream forms of Trypanosoma brucei
Summary
African sleeping sickness and leishmaniasis continue to cause significant public health problems. We reported the synthesis and trypanocidal profile of new (E)-cinnamic N-acylhydrazones (NAH) These derivatives were evaluated against both amastigote and trypomastigote forms of Trypanosoma cruzi and lead us to identify two compounds that were approximately two times more active than the reference drug, i.e., benznidazole, and present with good selectivity index [11]. They’re different kinetoplastid pathogens have a similar genomic organization and cellular structures [12] This evolutionary resemblance and the previous results obtained by our research group with T. cruzi encouraged us to evaluate a series of fourteen of these derivatives upon axenic amastigote forms of Leishmania donovani and against bloodstream forms of Trypanosoma brucei.
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