The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis
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 para...
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The Journal of Infection in Developing Countries
2019-06-01
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| Series: | Journal of Infection in Developing Countries |
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| Online Access: | https://jidc.org/index.php/journal/article/view/10622 |
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| author | Miriam Rolón Alejandro Peixoto de Abreu Lima Cathia Coronel Maria Celeste Vega Enrique Pandolfi Antonieta Rojas de Arias |
| author_facet | Miriam Rolón Alejandro Peixoto de Abreu Lima Cathia Coronel Maria Celeste Vega Enrique Pandolfi Antonieta Rojas de Arias |
| author_sort | Miriam Rolón |
| collection | DOAJ |
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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.
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| format | Article |
| id | doaj-art-66b6fc1bd10d451ca354d76f31f76c65 |
| institution | OA Journals |
| issn | 1972-2680 |
| language | English |
| publishDate | 2019-06-01 |
| publisher | The Journal of Infection in Developing Countries |
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| series | Journal of Infection in Developing Countries |
| spelling | doaj-art-66b6fc1bd10d451ca354d76f31f76c652025-08-20T02:27:05ZengThe Journal of Infection in Developing CountriesJournal of Infection in Developing Countries1972-26802019-06-01130610.3855/jidc.10622The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensisMiriam Rolón0Alejandro Peixoto de Abreu Lima1Cathia Coronel2Maria Celeste Vega3Enrique Pandolfi4Antonieta Rojas de Arias5Centro para el Desarrollo de la Investigación Científica (CEDIC) (Diaz Gil Medicina laboratorial/FMB), Asunción, ParaguayDepartamento de Química Orgánica, Facultad de Química, Universidad de la República, Montevideo, UruguayCentro para el Desarrollo de la Investigación Científica (CEDIC) (Diaz Gil Medicina laboratorial/FMB), Asunción, ParaguayCentro para el Desarrollo de la Investigación Científica (CEDIC) (Diaz Gil Medicina laboratorial/FMB), Asunción, ParaguayDepartamento de Química Orgánica, Facultad de Química, Universidad de la República, Montevideo, UruguayCentro para el Desarrollo de la Investigación Científica (CEDIC) (Diaz Gil Medicina laboratorial/FMB), Asunción, Paraguay 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. https://jidc.org/index.php/journal/article/view/10622Phenolic derivativesTrypanosome cruziLeishmania infantumLeishmania braziliensisAntiprotozoal activity |
| spellingShingle | Miriam Rolón Alejandro Peixoto de Abreu Lima Cathia Coronel Maria Celeste Vega Enrique Pandolfi Antonieta Rojas de Arias The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis Journal of Infection in Developing Countries Phenolic derivatives Trypanosome cruzi Leishmania infantum Leishmania braziliensis Antiprotozoal activity |
| title | The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis |
| title_full | The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis |
| title_fullStr | The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis |
| title_full_unstemmed | The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis |
| title_short | The efficacy of new 2,5-dihydroxybenzyl derivatives against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis |
| title_sort | efficacy of new 2 5 dihydroxybenzyl derivatives against trypanosoma cruzi leishmania infantum and leishmania braziliensis |
| topic | Phenolic derivatives Trypanosome cruzi Leishmania infantum Leishmania braziliensis Antiprotozoal activity |
| url | https://jidc.org/index.php/journal/article/view/10622 |
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