Following our search for antimalarial compounds, novel series of piperazinylalcohol pyrrolo[
1,2-a]quinoxaline derivatives 1-2 were synthesized from 2-nitroaniline or 2-amino-3-
nitrophenol and tested for in vitro activity upon the intraerythrocytic stage of W2 and 3D7 Plasmodium
falciparum strains. Biological results showed good antimalarial activity with IC50 ranging from
0.3 to 21.1 µM. In attempting to investigate the large broad-spectrum antiprotozoal activities of these
pyrrolo[1,2-a]quinoxaline derivatives, their properties toward the promastigote form of Leishmania
donovani were also investigated and revealed their selective antiplasmodial profile. In parallel, the in
vitro cytotoxicity of these molecules was assessed on the human HepG2 cell line. Structure-activity
relationships of these new synthetic compounds are here discussed.
Keywords: Antimalarial activity, pyrrolo[1, 2-a]quinoxaline, synthesis, antileishmanial activity.
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