English   español  
Por favor, use este identificador para citar o enlazar a este item: http://hdl.handle.net/10261/171242
COMPARTIR / IMPACTO:
Estadísticas
logo share SHARE logo core CORE   Add this article to your Mendeley library MendeleyBASE

Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL
Exportar a otros formatos:
Título

Antichagasic, Leishmanicidal, and Trichomonacidal Activity of 2-Benzyl-5-nitroindazole-Derived Amines

AutorFonseca-Berzal, Cristina; Ibáñez-Escribano, Alexandra; Vela, Nerea; Cumella, José; Nogal-Ruiz, Juan José; Escario, José Antonio; da Silva, P. B.; Soeiro, M. N. C.; Sifontes-Rodríguez, S; Meneses-Marcel, Alfredo; Gómez-Barrio, Alicia; Arán, Vicente J.
Palabras claveTrypanosomiasis
Nitrogen heterocycles
Leishmaniasis
Antiprotozoal agents
Trichomoniasis
Fecha de publicación2018
EditorWiley-VCH
CitaciónChemMedChem 13: 1246-1259 (2018)
ResumenThree different series of new 5-nitroindazole derivatives—1-(ω-aminoalkyl)-2-benzylindazolin-3-ones (series A; ten compounds), 3-(ω-aminoalkoxy)-2-benzylindazoles (series B; four compounds) and 3-alkylamino-2-benzylindazoles (series C; five compounds)—have been synthesized and evaluated against the protozoan parasites Trypanosoma cruzi, Leishmania amazonensis, and Trichomonas vaginalis: etiological agents of Chagas disease, cutaneous leishmaniasis, and trichomoniasis, respectively. Many indazoles of series A, B, and C were efficient against T. cruzi. Some compounds in series A, after successfully passing the preliminary screening for epimastigotes, exhibited activity values against amastigotes of several T. cruzi strains that were better than or similar to those shown by the reference drug benznidazole and displayed low nonspecific toxicity against mammalian cells. On the other hand, preliminary studies against promastigotes of L. amazonensis showed high leishmanicidal activity for some derivatives of series A and C. With regard to activity against T. vaginalis, some indazoles of series B and C were rather efficient against trophozoites of a metronidazole-sensitive isolate and showed low nonspecific toxicities toward Vero cell cultures. Additionally, some of these compounds displayed similar activity against metronidazole-sensitive and resistant isolates, showing the absence of cross-resistance between these derivatives and the reference drug.
Versión del editorhttp://dx.doi.org/10.1002/cmdc.201800084
URIhttp://hdl.handle.net/10261/171242
Identificadoresdoi: 10.1002/cmdc.201800084
issn: 1860-7179
e-issn: 1860-7187
Aparece en las colecciones: (IQM) Artículos
Ficheros en este ítem:
Fichero Descripción Tamaño Formato  
accesoRestringido.pdf15,38 kBAdobe PDFVista previa
Visualizar/Abrir
Mostrar el registro completo
 

Artículos relacionados:


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