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First-Row Transition 7-Oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes: Antiparasitic Activity and Release Studies

Leishmaniasis and Chagas disease are still considered neglected illnesses due to the lack of investment in research, despite the fact that almost one million new cases are reported every year. Four 7-oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine (HftpO) first-row transition complexes (Cu, Co, Ni, Zn)...

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Autores principales: Martín-Montes, Álvaro, Jimenez-Falcao, Sandra, Gómez-Ruiz, Santiago, Marín, Clotilde, Mendez-Arriaga, José M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10610057/
https://www.ncbi.nlm.nih.gov/pubmed/37895851
http://dx.doi.org/10.3390/ph16101380
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author Martín-Montes, Álvaro
Jimenez-Falcao, Sandra
Gómez-Ruiz, Santiago
Marín, Clotilde
Mendez-Arriaga, José M.
author_facet Martín-Montes, Álvaro
Jimenez-Falcao, Sandra
Gómez-Ruiz, Santiago
Marín, Clotilde
Mendez-Arriaga, José M.
author_sort Martín-Montes, Álvaro
collection PubMed
description Leishmaniasis and Chagas disease are still considered neglected illnesses due to the lack of investment in research, despite the fact that almost one million new cases are reported every year. Four 7-oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine (HftpO) first-row transition complexes (Cu, Co, Ni, Zn) have been studied for the first time in vitro against five different species of Leishmania spp. (L. infantum, L. braziliensis, L. donovani, L. peruviana and L. mexicana) as well as Trypanosoma cruzi, showing higher efficacy than the reference commercial drugs. UV and luminescence properties were also evaluated. As a proof of concept, anchoring of a model high-effective-metal complex as an antiparasitic agent on silica nanoparticles was carried out for the first time, and drug-release behaviour was evaluated, assessing this new approach for drug vehiculation.
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spelling pubmed-106100572023-10-28 First-Row Transition 7-Oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes: Antiparasitic Activity and Release Studies Martín-Montes, Álvaro Jimenez-Falcao, Sandra Gómez-Ruiz, Santiago Marín, Clotilde Mendez-Arriaga, José M. Pharmaceuticals (Basel) Article Leishmaniasis and Chagas disease are still considered neglected illnesses due to the lack of investment in research, despite the fact that almost one million new cases are reported every year. Four 7-oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine (HftpO) first-row transition complexes (Cu, Co, Ni, Zn) have been studied for the first time in vitro against five different species of Leishmania spp. (L. infantum, L. braziliensis, L. donovani, L. peruviana and L. mexicana) as well as Trypanosoma cruzi, showing higher efficacy than the reference commercial drugs. UV and luminescence properties were also evaluated. As a proof of concept, anchoring of a model high-effective-metal complex as an antiparasitic agent on silica nanoparticles was carried out for the first time, and drug-release behaviour was evaluated, assessing this new approach for drug vehiculation. MDPI 2023-09-28 /pmc/articles/PMC10610057/ /pubmed/37895851 http://dx.doi.org/10.3390/ph16101380 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Martín-Montes, Álvaro
Jimenez-Falcao, Sandra
Gómez-Ruiz, Santiago
Marín, Clotilde
Mendez-Arriaga, José M.
First-Row Transition 7-Oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes: Antiparasitic Activity and Release Studies
title First-Row Transition 7-Oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes: Antiparasitic Activity and Release Studies
title_full First-Row Transition 7-Oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes: Antiparasitic Activity and Release Studies
title_fullStr First-Row Transition 7-Oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes: Antiparasitic Activity and Release Studies
title_full_unstemmed First-Row Transition 7-Oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes: Antiparasitic Activity and Release Studies
title_short First-Row Transition 7-Oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes: Antiparasitic Activity and Release Studies
title_sort first-row transition 7-oxo-5-phenyl-1,2,4-triazolo[1,5-a]pyrimidine metal complexes: antiparasitic activity and release studies
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10610057/
https://www.ncbi.nlm.nih.gov/pubmed/37895851
http://dx.doi.org/10.3390/ph16101380
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