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In vitro Leishmanicidal and Trypanosomicidal Properties of Imidazole‐Containing Azine and Benzoazine Derivatives
Leishmaniasis and Chagas diseases are two of the most important parasitic diseases in the world. Both belong to the category of Neglected Tropical Diseases, and they cannot be prevented by vaccination. Their treatments are founded in outdated drugs that possess many pernicious side‐effects and they&...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley and Sons Inc.
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9298202/ https://www.ncbi.nlm.nih.gov/pubmed/34665510 http://dx.doi.org/10.1002/cmdc.202100413 |
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author | Martín‐Montes, Álvaro Kolodová, Kristina Marín, Clotilde Rosales‐Lombardo, María José Sánchez‐Moreno, Manuel de Andrés‐Gordo, Lucía Cano, Carmen Campayo, Lucrecia Gómez‐Muñoz, Alberto Sanz, Ana M. Yunta, María J. R. |
author_facet | Martín‐Montes, Álvaro Kolodová, Kristina Marín, Clotilde Rosales‐Lombardo, María José Sánchez‐Moreno, Manuel de Andrés‐Gordo, Lucía Cano, Carmen Campayo, Lucrecia Gómez‐Muñoz, Alberto Sanz, Ana M. Yunta, María J. R. |
author_sort | Martín‐Montes, Álvaro |
collection | PubMed |
description | Leishmaniasis and Chagas diseases are two of the most important parasitic diseases in the world. Both belong to the category of Neglected Tropical Diseases, and they cannot be prevented by vaccination. Their treatments are founded in outdated drugs that possess many pernicious side‐effects and they're not easy to administer. With the aim of discovering new compounds that could serve as anti‐trypanosomal drugs, an antiparasitic study of a synthetic compound family has been conducted. A series of new 1,4‐bis(alkylamino)‐ and 1‐alkylamino‐4‐chloroazine and benzoazine derivatives 1–4 containing imidazole rings have been synthesized and identified. Their structures showed a possible interest based on previous work. Their in vitro anti‐Leishmania infantum, anti‐L. braziliensis, anti‐L. donovani and anti‐T. cruzi activity were tested, as well as the inhibition of Fe‐SOD enzymes. It was found that some of them exhibited quite relevant values indicative of being worthy of future more detailed studies, as most of them showed activity to more than only one parasite species, especially compound 3 c was active for the three studied Leishmania species and also for T. cruzi, which is a very interesting trait as it covers a wide spectrum. |
format | Online Article Text |
id | pubmed-9298202 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | John Wiley and Sons Inc. |
record_format | MEDLINE/PubMed |
spelling | pubmed-92982022022-07-21 In vitro Leishmanicidal and Trypanosomicidal Properties of Imidazole‐Containing Azine and Benzoazine Derivatives Martín‐Montes, Álvaro Kolodová, Kristina Marín, Clotilde Rosales‐Lombardo, María José Sánchez‐Moreno, Manuel de Andrés‐Gordo, Lucía Cano, Carmen Campayo, Lucrecia Gómez‐Muñoz, Alberto Sanz, Ana M. Yunta, María J. R. ChemMedChem Full Papers Leishmaniasis and Chagas diseases are two of the most important parasitic diseases in the world. Both belong to the category of Neglected Tropical Diseases, and they cannot be prevented by vaccination. Their treatments are founded in outdated drugs that possess many pernicious side‐effects and they're not easy to administer. With the aim of discovering new compounds that could serve as anti‐trypanosomal drugs, an antiparasitic study of a synthetic compound family has been conducted. A series of new 1,4‐bis(alkylamino)‐ and 1‐alkylamino‐4‐chloroazine and benzoazine derivatives 1–4 containing imidazole rings have been synthesized and identified. Their structures showed a possible interest based on previous work. Their in vitro anti‐Leishmania infantum, anti‐L. braziliensis, anti‐L. donovani and anti‐T. cruzi activity were tested, as well as the inhibition of Fe‐SOD enzymes. It was found that some of them exhibited quite relevant values indicative of being worthy of future more detailed studies, as most of them showed activity to more than only one parasite species, especially compound 3 c was active for the three studied Leishmania species and also for T. cruzi, which is a very interesting trait as it covers a wide spectrum. John Wiley and Sons Inc. 2021-10-19 2021-12-06 /pmc/articles/PMC9298202/ /pubmed/34665510 http://dx.doi.org/10.1002/cmdc.202100413 Text en © 2021 The Authors. ChemMedChem published by Wiley-VCH GmbH https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the terms of the http://creativecommons.org/licenses/by-nc-nd/4.0/ (https://creativecommons.org/licenses/by-nc-nd/4.0/) License, which permits use and distribution in any medium, provided the original work is properly cited, the use is non‐commercial and no modifications or adaptations are made. |
spellingShingle | Full Papers Martín‐Montes, Álvaro Kolodová, Kristina Marín, Clotilde Rosales‐Lombardo, María José Sánchez‐Moreno, Manuel de Andrés‐Gordo, Lucía Cano, Carmen Campayo, Lucrecia Gómez‐Muñoz, Alberto Sanz, Ana M. Yunta, María J. R. In vitro Leishmanicidal and Trypanosomicidal Properties of Imidazole‐Containing Azine and Benzoazine Derivatives |
title |
In vitro Leishmanicidal and Trypanosomicidal Properties of Imidazole‐Containing Azine and Benzoazine Derivatives |
title_full |
In vitro Leishmanicidal and Trypanosomicidal Properties of Imidazole‐Containing Azine and Benzoazine Derivatives |
title_fullStr |
In vitro Leishmanicidal and Trypanosomicidal Properties of Imidazole‐Containing Azine and Benzoazine Derivatives |
title_full_unstemmed |
In vitro Leishmanicidal and Trypanosomicidal Properties of Imidazole‐Containing Azine and Benzoazine Derivatives |
title_short |
In vitro Leishmanicidal and Trypanosomicidal Properties of Imidazole‐Containing Azine and Benzoazine Derivatives |
title_sort | in vitro leishmanicidal and trypanosomicidal properties of imidazole‐containing azine and benzoazine derivatives |
topic | Full Papers |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9298202/ https://www.ncbi.nlm.nih.gov/pubmed/34665510 http://dx.doi.org/10.1002/cmdc.202100413 |
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