RT info:eu-repo/semantics/article
T1 The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis
A1 Rolón, Miriam Soledad
A1 Peixoto de Abreu Lima, Alejandro
A1 Coronel, Cathia Cecilia
A1 Vega Gómez, María Celeste
A1 Pandolfi, Enrique
A1 Rojas de Arias, Gladys Antonieta
AB 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.
PB The Journal of Infection in Developing Countries
SN 1972-2680
YR 2019
FD 2019-06-30
LK http://hdl.handle.net/20.500.14066/4431
UL http://hdl.handle.net/20.500.14066/4431
LA eng
NO Rolón, M., Peixoto de Abreu Lima, A., Coronel, C., Vega, M. C., Pandolfi, E., & Rojas de Arias, A. (2019). The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis. The Journal of Infection in Developing Countries, 13(06), 565-576. https://doi.org/10.3855/jidc.10622
NO Corresponding author:Enrique Pandolfi, Professor PhDPrincipal Investigator of the Organic Chemistry DepartmentAvenida General Flores 2124, CP 11800, Montevideo, Uruguay.Tel.: +598-2924-7881Fax: +598-2924-1906Email: epandolf@fq.edu.uyAntonieta Rojas de Arias, PhDTechnical Director of the Center for Development and Scientific Research (CEDIC)Manduvirá 635, CP 1255, Asunción, Paraguay.Tel.: +595-981-504996Fax: +595-21-441513Email: rojasdearias@gmail.com
NO Consejo Nacional de Ciencia y Tecnología
DS MINDS@UW
RD 16-jul-2024