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9-Arylpurines as a Novel Class of Enterovirus Inhibitors

AuthorsAguado, Leire ; Thibaut, Hendrik Jan; Priego, Eva María ; Jimeno, M. Luisa ; Camarasa Rius, María José ; Neyts, Johan; Pérez Pérez, María Jesús
Issue Date2010
PublisherAmerican Chemical Society
CitationJournal of Medicinal Chemistry 53 : 316-324 (2010)
AbstractHere wereporton a novel class ofenterovirus inhibitors thatcan bestructurallydescribedas9-arylpurines. These compounds elicit activityagainst a varietyof enteroviruse s in the low μMrange including Coxsackie virus A16, A21, A24, Coxsackie virus B3, and echovirus 9. Structure-activity relationship(SAR) studies indicatethat achlorine orbromine atomisrequired atposition 6of the purinering for antiviralactivity. The most selective compounds in this series inhibited Coxsackie virus B3 replication in a dose-dependent manner withEC50 values around5-8μM. No toxicity ondifferent celllines wasobservedatconcentrations up to 250 μM. Moreover, no cross-resistance to TBZE-029 and TTP-8307 CVB3 resistant strains was detected.
Publisher version (URL)http://dx.doi.org/10.1021/jm901240p
Appears in Collections:(CENQUIOR) Artículos
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