1'-C-氰基-2'-氟-2'-C-甲基嘧啶核苷作为丙型肝炎病毒聚合酶抑制剂的合成与表征
Synthesis and characterization of 1'-C-cyano-2'-fluoro-2'-C-methyl pyrimidine nucleosides as HCV polymerase inhibitors.
作者信息
Kirschberg Thorsten A, Mish Michael R, Zhang Lijun, Squires Neil H, Wang Ke-Yu, Cho Aesop, Feng Joy Y, Fenaux Martijn, Babusis Darius, Park Yeojin, Ray Adrian S, Kim Choung U
机构信息
Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94044, USA.
出版信息
Bioorg Med Chem Lett. 2015 Mar 1;25(5):1040-3. doi: 10.1016/j.bmcl.2015.01.021. Epub 2015 Jan 17.
The first synthesis of 1'-C-CN, 2'-F, 2'-C-Me pyrimidines is described. Anti-HCV activity was assessed and compared to the 1'-C-CN, 2'-C-Me as well as the 2'-F, 2'-C-Me pyrimidines. A phosphoramidate prodrug of the cytidine derivative showed activity in the low micromolar range against HCV replicons.
描述了1'-C-CN、2'-F、2'-C-甲基嘧啶的首次合成。评估了其抗丙型肝炎病毒（HCV）活性，并与1'-C-CN、2'-C-甲基以及2'-F、2'-C-甲基嘧啶进行了比较。胞苷衍生物的磷酰胺酯前药对HCV复制子显示出低微摩尔范围的活性。
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