Key result
9-arylpurines inhibited Coxsackie virus B3 replication in a dose-dependent manner with EC50 values of 5-8 microM, with no observed toxicity on cell lines up to 250 microM.
Why the study?
Do 9-arylpurines inhibit enterovirus replication in vitro?
Do 9-arylpurines inhibit enterovirus replication in vitro?
Effect estimate: EC50 5-8 microM
9-arylpurines represent a novel class of enterovirus inhibitors with low micromolar activity and no observed in vitro toxicity.
Supports further development of 9-arylpurines as enterovirus antivirals; leaves open in vivo efficacy and clinical translation.
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 microM 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 EC(50) values around 5-8 microM. No toxicity on different cell lines was observed at concentrations up to 250 microM. Moreover, no cross-resistance to TBZE-029 and TTP-8307 CVB3 resistant strains was detected.
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Aguado et al. (2009) studied Enterovirus infection. 9-arylpurines was evaluated on Coxsackie virus B3 replication inhibition (EC50 5-8 microM). 9-arylpurines inhibited Coxsackie virus B3 replication in a dose-dependent manner with EC50 values of 5-8 microM, with no observed toxicity on cell lines up to 250 microM.
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