Synthesis and antileishmanial activity of naphthoquinone-based hybrids

Introduction: leishmaniasis is a disease caused by protozoa of the genus Leishmania and considered endemic in 98 countries. Treatment with pentavalent antimonials has high toxicity, which motivates search for effective less toxic drugs. α- β-lapachones have shown different biological activities, including antiprotozoa. In recent studies, isonicotinoylhydrazone phthalazinylhydrazone groups were innovative development antileishmania Molecular hybridization strategy rational new prototypes, where main compound produced through appropriate binding pharmacophoric subunits. Aims: to synthesize four hybrids β-lapachones, together determine activity against promastigotic forms L. amazonensis, infantum major. Results: β-lapachone derivatives more active all tested leishmania species. ΒACIL (IC50 0.044µM) βHDZ 0.023µM) showed 15-fold higher than amphotericin B. The selectivity index exhibited compounds indicates greater safety vertebrate host cells. Conclusion: results this work show that βACIL are promising molecules