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Efficient synthesis and anti-enteroviral activity of 9-arylpurines

AuthorsAguado, Leire ; Canela, María-Dolores ; Thibaut, Hendrik Jan; Priego, Eva María ; Camarasa Rius, María José ; Leyssen, Pieter; Neyts, Johan; Peréz-Pérez, María-Jesús
Microwave-assisted synthesis
Coxsackie virus B3
Issue Date2012
CitationEuropean Journal of Medicinal Chemistry 49 : 279–288 (2012)
AbstractTo further explore the anti-enteroviral activity of 9-aryl-6-chloropurines, three different series of compounds with a dialkylamino, (alkyl)amido, or oxazolidinone substituent at the aryl ring have been synthesized, in most cases with the aid of microwave-assisted synthesis. The resulting compounds efficiently inhibit Coxsackie virus type B3 (CVB3) replication with EC50 values varying from 3 to 15 mM, and with no significant toxicity in Vero cells. The most potent compounds also selectively inhibit the replication of other enteroviruses including Coxsackie virus B4 and Echo virus 11. The cross-resistance studies performed with different 9-aryl-6-chloropurines indicate that they all belong to the same pharmacological family and differ from other CVB3 drugs such as enviroxime.
Publisher version (URL)http://dx.doi.org/10.1016/j.ejmech.2012.01.022,
Appears in Collections:(IQM) Artículos
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