English   español  
Por favor, use este identificador para citar o enlazar a este item: http://hdl.handle.net/10261/98402
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:

Identification of [1,2,3]triazolo[4,5-d ]pyrimidin-7(6H)-ones as novel inhibitors of chikungunya virus replication

AutorGigante, Alba ; Canela, María-Dolores ; Delang, Leen; Priego, Eva María ; Camarasa Rius, María José ; Querat, Guilles; Neyts, Johan; Leyssen, Pieter; Peréz-Pérez, María-Jesús
Fecha de publicación2014
EditorAmerican Chemical Society
CitaciónJournal of Medicinal Chemistry 57: 4000- 4008 (2014)
ResumenChikungunya virus (CHIKV) is a re-emerging Alphavirus that is transmitted to humans by Aedes mosquitoes. Currently, there are still no drugs or vaccines available for the treatment or prevention of this disease. Although traditionally restricted to Africa and Asia, the adaptation of the virus to Aedes albopictus, a mosquito species with an almost worldwide distribution, has contributed to the geographical spread of this virus in the past decade. Here, we report on a new family of compounds named [1,2,3]triazolo[4,5-d]pyrimidin- 7(6H)-ones that inhibit CHIKV replication in the low micromolar range with no toxicity to the host (Vero) cells. The most potent compound in this series has an EC50 value below 1 μM with no cytotoxicity detected up to 668 μM, therefore affording a selectivity index greater than 600. Interestingly, the compounds have little or no antiviral activity on the replication of other members of the Togaviridae family. The exploration and study of this class of selective inhibitors of CHIKV replication will contribute to deeper insights into the CHIKV life cycle and may be a first step toward the development of a clinical drug candidate. © 2014 American Chemical Society.
Versión del editorhttp://dx.doi.org/10.1021/jm401844c
Identificadoresdoi: 10.1021/jm401844c
issn: 0022-2623
e-issn: 1520-4804
Aparece en las colecciones: (IQM) Artículos
Ficheros en este ítem:
No hay ficheros asociados a este ítem.
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.