侧链带有膦酰甲氧基的无环2'-氮杂核苷的合成及抗病毒活性评价
Synthesis and antiviral activity evaluation of acyclic 2'-azanucleosides bearing a phosphonomethoxy function in the side chain.
作者信息
Koszytkowska-Stawińska Mariola, De Clercq Erik, Balzarini Jan
机构信息
Faculty of Chemistry, Warsaw University of Technology, ul. Noakowskiego 3, 00-664 Warszawa, Poland.
出版信息
Bioorg Med Chem. 2009 Jun 1;17(11):3756-62. doi: 10.1016/j.bmc.2009.04.054. Epub 2009 May 3.
Abstract
Acyclic 2'-azanucleosides with a phosphonomethoxy function in the side chain were obtained by coupling of diethyl {2-[N-(pivaloyloxymethyl)-N-(p-toluenesulfonyl)amino]ethoxymethyl}phosphonate with the pyrimidine nucleobases via the Vorbrüggen-type protocol. The compounds were evaluated in vitro for activity against a broad variety of RNA and DNA viruses.
摘要
通过二乙基{2-[N-(新戊酰氧基甲基)-N-(对甲苯磺酰基)氨基]乙氧基甲基}膦酸酯与嘧啶核碱基经由Vorbrüggen型反应方案进行偶联，得到了侧链带有膦酰甲氧基官能团的无环2'-氮杂核苷。对这些化合物进行了体外评估，以检测其对多种RNA和DNA病毒的活性。
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