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Revista Colombiana de Ciencias Químico - Farmacéuticas
Print version ISSN 0034-7418On-line version ISSN 1909-6356
Abstract
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. https://doi.org/10.15446/rcciquifa.v50n2.92861.
Introduction:
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.
Aims:
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.
Results:
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.
Conclusion:
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.