The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis

  • Miriam Rolón Centro para el Desarrollo de la Investigación Científica (CEDIC) (Diaz Gil Medicina laboratorial/FMB), Asunción, Paraguay
  • Alejandro Peixoto de Abreu Lima Departamento de Química Orgánica, Facultad de Química, Universidad de la República, Montevideo, Uruguay
  • Cathia Coronel Centro para el Desarrollo de la Investigación Científica (CEDIC) (Diaz Gil Medicina laboratorial/FMB), Asunción, Paraguay
  • Maria Celeste Vega Centro para el Desarrollo de la Investigación Científica (CEDIC) (Diaz Gil Medicina laboratorial/FMB), Asunción, Paraguay
  • Enrique Pandolfi Departamento de Química Orgánica, Facultad de Química, Universidad de la República, Montevideo, Uruguay
  • Antonieta Rojas de Arias Centro para el Desarrollo de la Investigación Científica (CEDIC) (Diaz Gil Medicina laboratorial/FMB), Asunción, Paraguay
Keywords: Phenolic derivatives, Trypanosome cruzi, Leishmania infantum, Leishmania braziliensis, Antiprotozoal activity

Abstract

Introduction: Chagas disease and Leishmaniasis are among the most important parasitic diseases. They are considered to be within the most relevant group of neglected tropical diseases and have been included as priorities for searching new drugs due to their several treatment limitations. These parasitic diseases caused by flagellated protozoans affect more than 20 million people predominantly in developing countries.

Methodology: In this study, we prepared a series of 2-substituted 1,4-benzenediols by an efficient, green, and lithium salt-free synthesis in water/ethanol as solvent to test their anti-parasitic activity. All 36 phenolic derivatives were evaluated in vitro for their activity against T. cruzi epimastigotes, L. infantum, and L. braziliensis promastigotes, as well as their cytotoxicity on macrophage and fibroblast cell lines.

Results: Based on the results obtained, the compounds that presented a methyl, trifluoromethyl or bromo group at the para-position of the second benzene ring were found the most active analogs, with higher selective index values on the three parasites assayed.

Conclusion: This evidence suggests that the anti-parasitic activity observed in these analogs is affected by the size of the group at the 4-position of the second ring, but not related with electronic factors.This study identified hit compounds with the potential to target several kinetoplastid parasites.

Published
2019-06-30
How to Cite
1.
Rolón M, Peixoto de Abreu Lima A, Coronel C, Vega MC, Pandolfi E, Rojas de Arias A (2019) The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis. J Infect Dev Ctries 13:565-576. doi: 10.3855/jidc.10622
Section
Original Articles