Por favor, use este identificador para citar o enlazar a este item: http://hdl.handle.net/10261/194887
COMPARTIR / EXPORTAR:
logo share SHARE logo core CORE BASE
Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL | DATACITE

Invitar a revisión por pares abierta
Título

In vitro assessment of 3-alkoxy-5-nitroindazole-derived ethylamines and related compounds as potential antileishmanial drugs

AutorMartín-Montes, Á.; Aguilera-Venegas, Benjamín; Morales-Martín, Rosa Mª; Martín-Escolano, R.; Zamora-Ledesma, S.; Marín, C.; Arán, Vicente J. CSIC ORCID; Sánchez-Moreno, Manuel
Palabras claveIndazoles
Nitroheterocycles
Antiprotozoal agents
Drug discovery
Leishmania
Fecha de publicación2019
EditorAcademic Press
CitaciónBioorganic Chemistry 92 (2019)
ResumenLeishmaniasis is a widespread neglected tropical disease complex that is responsible of one million new cases per year. Current treatments are outdated and pose many problems that new drugs need to overcome. With the goal of developing new, safe, and affordable drugs, we have studied the in vitro activity of 12 different 5-nitroindazole derivatives that showed previous activity against different strains of Trypanosoma cruzi in a previous work. T. cruzi belongs to the same family as Leishmania spp., and treatments for the disease it produces also needs renewal. Among the derivatives tested, compounds 1, 2, 9, 10, 11, and 12 showed low J774.2 macrophage toxicity, while their effect against both intracellular and extracellular forms of the studied parasites was higher than the ones found for the reference drug Meglumine Antimoniate (Glucantime®). In addition, their Fe-SOD inhibitory effect, the infection rates, metabolite alteration, and mitochondrial membrane potential of the parasites treated with the selected drugs were studied in order to gain insights into the action mechanism, and the results of these tests were more promising than those found with glucantime, as the leishmanicidal effect of these new drug candidates was higher. The promising results are encouraging to test these derivatives in more complex studies, such as in vivo studies and other experiments that could find out the exact mechanism of action.
Versión del editorhttp://dx.doi.org/10.1016/j.bioorg.2019.103274
URIhttp://hdl.handle.net/10261/194887
DOI10.1016/j.bioorg.2019.103274
Identificadoresdoi: 10.1016/j.bioorg.2019.103274
issn: 0045-2068
e-issn: 1090-2120
Aparece en las colecciones: (ICTP) Artículos




Ficheros en este ítem:
Fichero Descripción Tamaño Formato
accesoRestringido.pdf15,38 kBAdobe PDFVista previa
Visualizar/Abrir
Mostrar el registro completo

CORE Recommender

SCOPUSTM   
Citations

4
checked on 08-mar-2024

WEB OF SCIENCETM
Citations

4
checked on 29-feb-2024

Page view(s)

200
checked on 29-mar-2024

Download(s)

25
checked on 29-mar-2024

Google ScholarTM

Check

Altmetric

Altmetric


NOTA: Los ítems de Digital.CSIC están protegidos por copyright, con todos los derechos reservados, a menos que se indique lo contrario.