6-Hydrazinopurine 2′-methyl ribonucleosides and their 5′-monophosphate prodrugs as potent hepatitis C virus inhibitors
6-Hydrazinopurine 2′-methyl ribonucleosides and their 5′-monophosphate prodrugs as potent hepatitis C virus inhibitors
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DOI：
10.1016/j.bmcl.2007.02.029
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发表时间：
2007-05-01
影响因子：
2.7
通讯作者：
Girardet, Jean-Luc
中科院分区：
文献类型：
--
作者：
Gunic, Esmir;Chow, Suetying;Girardet, Jean-Luc
合成了一系列6-肼嘌呤2'-甲基核糖核苷并测试了其对丙型肝炎病毒（HCV）的抑制活性。这些核苷缺乏抗病毒活性与腺苷激酶的亲和力差有关，这促使我们合成了它们的几种 5'-单磷酸前药。与母体核苷相比，其中一些前药的抗 HCV 活性提高了 1000 倍以上（EC50 为 24 μM，母体为 92 μM）。 (C) 2007 Elsevier Ltd. 保留所有权利。
A series of 6-hydrazinopurine 2 '-methyl ribonucleosides was synthesized and tested for its inhibitory activity against the hepatitis C virus (HCV). The lack of antiviral activity of these nucleosides was associated with a poor affinity for adenosine kinase, which prompted us to synthesize several of their 5 '-monophosphate prodrugs. Some of these prodrugs exhibited more than 1000-fold improvement in anti-HCV activity when compared to their parent nucleosides (EC50 of 24 mu M vs 92 mu M for the parent). (C) 2007 Elsevier Ltd. All rights reserved.