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9-Arylpurines as a Novel Class of Enterovirus Inhibitors
Ist Teil von
Journal of medicinal chemistry, 2010-01, Vol.53 (1), p.316-324
Ort / Verlag
Columbus, OH: American Chemical Society
Erscheinungsjahr
2010
Link zum Volltext
Quelle
MEDLINE
Beschreibungen/Notizen
Here we report on a novel class of enterovirus inhibitors that can be structurally described as 9-arylpurines. These compounds elicit activity against a variety of enteroviruses in the low μM range including Coxsackie virus A16, A21, A24, Coxsackie virus B3, and echovirus 9. Structure−activity relationship (SAR) studies indicate that a chlorine or bromine atom is required at position 6 of the purine ring for antiviral activity. The most selective compounds in this series inhibited Coxsackie virus B3 replication in a dose-dependent manner with EC50 values around 5−8 μM. No toxicity on different cell lines was observed at concentrations up to 250 μM. Moreover, no cross-resistance to TBZE-029 and TTP-8307 CVB3 resistant strains was detected.