碱基功能化碳环核苷：抗病毒活性的设计、合成及作用机制
Base-functionalized carbocyclic nucleosides: design, synthesis, and mechanism of antiviral activity.
作者信息
Nair Vasu, Zhang Fan, Ma Xiaohui, Bonsu Eric
机构信息
Department of Pharmaceutical and Biomedical Sciences and the Center for Drug Discovery, University of Georgia, Athens, Georgia, USA.
出版信息
Nucleosides Nucleotides Nucleic Acids. 2009 May;28(5):408-23. doi: 10.1080/15257770903044465.
Abstract
New carbocyclic ribonucleosides with unsaturated groups at the C-2 position of the nucleobase were designed as potential RNA antiviral compounds. The design was based on the expectation that the monophosphates of these compounds would be inhibitors of the enzyme, IMPDH. Appropriate methodologies were developed to achieve the target molecules. Results from the initial in vitro antiviral studies are mentioned. The IMPDH-associated mechanism of the antiviral activity of the most active compound is supported by enzyme inhibition studies.
摘要
设计了在核苷碱基的C-2位带有不饱和基团的新型碳环核糖核苷作为潜在的RNA抗病毒化合物。该设计基于这样的预期，即这些化合物的单磷酸盐将是IMP脱氢酶的抑制剂。开发了适当的方法来合成目标分子。文中提到了初步体外抗病毒研究的结果。酶抑制研究支持了最具活性化合物抗病毒活性的IMP脱氢酶相关机制。
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