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Title

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

AuthorsGigante, Alba ; Canela, María-Dolores ; Delang, Leen; Priego, Eva María ; Camarasa Rius, María José ; Querat, Guilles; Neyts, Johan; Leyssen, Pieter; Peréz-Pérez, María-Jesús
Issue Date2014
PublisherAmerican Chemical Society
CitationJournal of Medicinal Chemistry 57: 4000- 4008 (2014)
AbstractChikungunya 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.
Publisher version (URL)http://dx.doi.org/10.1021/jm401844c
URIhttp://hdl.handle.net/10261/98402
DOI10.1021/jm401844c
Identifiersdoi: 10.1021/jm401844c
issn: 0022-2623
e-issn: 1520-4804
Appears in Collections:(IQM) Artículos
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