New naphthoquinone derivatives were synthesized and assayed against bloodstream trypomastigote forms of
Trypanosoma cruzi, the etiological agent of Chagas’ disease. The compounds were rationalized based on hybrid
drugs and appear as important compounds against this parasite. From nor-lapachol were prepared five substituted
ortho-naphthofuranquinones, a non-substituted
para-naphthofuranquinone, a new oxyrane and an azide and from
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-lapachone a new non-substituted
para-naphthofuranquinone. Other five substituted
ortho-naphthofuranquinones recently designed as cytotoxic, were also evaluated. The most active compounds were the ortho naphthofuranquinones 3-(4-methoxyphenylamino)-2,3-dihydro-2,2-dimethylnaphtho[1,2-
b]furan-4,5-dione and 3-(3-nitrophenylamino)-2,3-dihydro-2,2-dimethylnaphtho[1,2-
b]furan-4,5-dione with
trypanocidal activity higher than that of benznidazole, the standard drug. The compounds were rationalized based on hybrid
drugs and appear as important compounds against
T. cruzi. The
trypanocidal activity of these substances endowed with redox properties representing a good starting point for a medicinal chemistry program aiming the chemotherapy of Chagas’ disease.