9-Arylpurines as a Novel Class of Enterovirus Inhibitors
9-Arylpurines as a Novel Class of Enterovirus Inhibitors
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DOI：
10.1021/jm901240p
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发表时间：
2010-01-14
影响因子：
7.3
通讯作者：
Perez-Perez, Maria-Jesus
中科院分区：
文献类型：
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作者：
Aguado, Leire;Thibaut, Hendrik Jan;Perez-Perez, Maria-Jesus
在这里，我们报告一类新的肠道病毒抑制剂，可以在结构上描述其9-芳基嘌呤。这些化合物在低μ M范围内引发抗多种肠道病毒的活性，包括科萨基病毒A16、A21、A24、科萨基病毒B3和埃可病毒9。构效关系（SAR）研究表明，它的抗病毒活性需要在嘌呤环的6位上的氯或溴原子。该系列中选择性最强的化合物以剂量依赖性方式抑制科萨基病毒B3复制，EC 50值约为5-8 μ M。在高达250 μ M的浓度下未观察到不同细胞系的毒性。此外，未检测到对TBZE-029和TTP-8307 CVB 3抗性菌株的交叉抗性。
Here we report on a novel class of enterovirus inhibitors that can be structurally described its 9-arylpurines. These compounds elicit activity against it variety of enteroviruses in the low mu M range including Coxsackie virus A16, A21, A24, Coxsackie Virus B3, and echovirus 9. Structure-activity relationship (SAR) studies indicate that it 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 it dose-dependent manner with EC50 values around 5-8 mu M. No toxicity oil different cell lines was observed at concentrations up to 250 mu M, Moreover, no cross-resistance to TBZE-029 and TTP-8307 CVB3 resistant strains was detected.