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Revista Colombiana de Ciencias Químico - Farmacéuticas

Print version ISSN 0034-7418On-line version ISSN 1909-6356


GUIMARAES, Délis Galvão et al. Synthesis and antileishmanial activity of naphthoquinone-based hybrids. Rev. colomb. cienc. quim. farm. [online]. 2021, vol.50, n.2, pp.505-521.  Epub Nov 05, 2021. ISSN 0034-7418.


Leishmaniasis is a disease caused by protozoa of the genus Leishmania and is considered endemic in 98 countries. Treatment with pentavalent antimonials has a high toxicity, which motivates the search for effective and less toxic drugs. α- and β-lapachones have shown different biological activities, including antiprotozoa. In recent studies, the isonicotinoylhydrazone and phthalazinylhydrazone groups were considered innovative in the development of antileishmania drugs. Molecular hybridization is a strategy for the rational development of new prototypes, where the main compound is produced through the appropriate binding of pharmacophoric subunits.


To synthesize four hybrids of α- and β-lapachones, together with the isonicotinoylhydrazone and phthalazinylhydrazone groups and to determine the antileishmania activity against the promastigotic forms of L. amazonensis, L. infantum and L. major.


β-lapachone derivatives were more active against all tested leishmania species. βACIL (IC50 0.044μM) and βHDZ (IC50 0.023μM) showed 15-fold higher activity than amphotericin B. The high selectivity index exhibited by the compounds indicates greater safety for vertebrate host cells.


The results of this work show that the hybrids βACIL and (3HDZ are promising molecules for the development of new antileishmania drugs.

Keywords : βlapachone; α-lapachone; molecular hybridization; hydralazine; isoniazid; hydrazone.

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