Services on Demand
Journal
Article
Indicators
- Cited by SciELO
- Access statistics
Related links
- Cited by Google
- Similars in SciELO
- Similars in Google
Share
Revista Colombiana de Ciencias Químico - Farmacéuticas
Print version ISSN 0034-7418On-line version ISSN 1909-6356
Abstract
SILVA, Adriano Olímpio da et al. Biological activities of 1,4-naphthoquinones derivatives against T. cruzi and L. amazonensis. Rev. colomb. cienc. quim. farm. [online]. 2022, vol.51, n.2, pp.752-786. Epub Dec 19, 2023. ISSN 0034-7418. https://doi.org/10.15446/rcciquifa.v51n2.98279.
Introduction:
Chagas disease and Leishmaniasis are neglected diseases caused by the Trypanosoma cruzi and kentoplastid parasites Leishmania spp. Parasitic diseases cause great impact on social and economic, affecting millions of people in the world and represent a major global health problem. In the search for new alternatives for the treatment of Leishmaniasis and Chagas disease, strategies have been used to discover new active molecules, because there is an urgent need for the development of new drugs. In this scenario, 1,4-naphthoquinones have shown notable activity in the context of neglected diseases.
Aim:
To synthesis of 1,4-naphthoquinones derivatives and evaluated these compounds against Trypanosoma cruzi epimastigotes, Leishmania promastigotes (Leishmania amazonensis) and cytotoxicity to LLCMK2 cells.
Results:
Nine 1,4-naphthoquinones derivatives were synthesized using 2-Bromo-1,4-naphthoquinone (1), 1,4-Naphthoquinone (5) and 2-Hydroxi-1,4-naphthoqui-none (9) as starting material. Derivative 6a exhibited excellent trypanocidal activity, IC50 of 0.25 ± 0.02 µM, superior potency compared with the reference drug Benznidazol. Besides, these compounds displayed low activity against promastigote from L. amazonensis.
Conclusion:
The results indicate that compound 6a may have potential for agent against Chagas disease.
Keywords : Naphthoquinone; Trypanosoma cruzi; Leishmania; Chagas diseases.