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新型取代 9-降冰片基嘌呤核苷及其抗 RNA 病毒活性。

Novel substituted 9-norbornylpurines and their activities against RNA viruses.

机构信息

Gilead Sciences & IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic.

出版信息

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1963-8. doi: 10.1016/j.bmcl.2012.01.040. Epub 2012 Jan 25.

Abstract

We report on the synthesis and the study of the structure-activity relationship of novel 9-norbornyl-6-chloropurine derivatives, which exert selective antiviral activity on the replication of Coxsackievirus B3. In particular, the synthetic approaches towards norbornyl derivatives bearing diverse side chains were studied. The main goal of the study was to determine the influence of the norbornane moiety substitution at positions 5' and 6' on selective antiviral activity with special regard to the liphophilicity profile of the substituent.

摘要

我们报告了新型 9-降冰片基-6-氯嘌呤衍生物的合成和构效关系研究,这些衍生物对柯萨奇病毒 B3 的复制具有选择性抗病毒活性。特别是,研究了带有不同侧链的降冰片衍生物的合成方法。该研究的主要目的是确定 5'和 6'位的降冰片烷部分取代对选择性抗病毒活性的影响,特别关注取代基的亲脂性特征。

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