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Título

Microwave-assisted synthesis of C-8 aryl and heteroaryl inosines and determination of their inhibitory activities against Plasmodium falciparum purine nucleoside phosphorylase

Autor Gigante, Alba ; Priego, Eva María ; Sánchez-Carrasco, Paula; Ruiz-Pérez, Luis Miguel; Vande Voorde, Johan; Camarasa Rius, María José ; Balzarini, Jan; González-Pacanowska, D.; Pérez Pérez, María Jesús
Palabras clave Inosine Phosphorylase
Microwave-assisted synthesis
Direct C-arylation
Antiviral
Phosphorylase
Fecha de publicación 2014
Citación European Journal of Medicinal Chemistry 82: 459- 465 (2014)
Resumen8-Arylinosines have been scarcely studied for therapeutic purposes, probably due to difficulties in their synthesis. The recently described direct arylation reaction at position 8 of purine nucleosides has been employed to synthesize a series of 8-aryl and 8-pyridylinosines. These compounds have been studied for hydrolytic stability and subjected to biological evaluation. Three compounds have shown a pronounced specific inhibition of Plasmodium falciparum-encoded purine nucleoside phosphorylase, an important target for antimalarial chemotherapy.
Versión del editorhtttp://dx.doi.org/10.1016/j.ejmech.2014.05.073
URI http://hdl.handle.net/10261/100907
DOI10.1016/j.ejmech.2014.05.073
Identificadoresdoi: 10.1016/j.ejmech.2014.05.073
issn: 0223-5234
e-issn: 1768-3254
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