2'-甲基胞苷新型磷酰胺酯前药作为丙型肝炎病毒NS5B聚合酶抑制剂的合成与评价
Synthesis and evaluation of novel phosphoramidate prodrugs of 2'-methyl cytidine as inhibitors of hepatitis C virus NS5B polymerase.
作者信息
Donghi Monica, Attenni Barbara, Gardelli Cristina, Marco Annalise Di, Fiore Fabrizio, Giuliano Claudio, Laufer Ralph, Leone Joseph F, Pucci Vincenzo, Rowley Michael, Narjes Frank
机构信息
Department of Medicinal Chemistry, IRBM-MRL Rome, Via Pontina Km 30,600, 00040 Pomezia (Rome), Italy.
出版信息
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1392-5. doi: 10.1016/j.bmcl.2009.01.035. Epub 2009 Jan 19.
A variety of new prodrugs of 2'-methyl cytidine based on acyloxy ethylamino phosphoramidates have been synthesized and tested in vitro and in vivo for their biological activity. Compared with the parent drug a 10- to 20-fold increase in formation of nucleotide triphosphate in rat and human hepatocytes could be achieved.
已经合成了多种基于酰氧基乙氨基磷酸酯的2'-甲基胞苷前药，并在体外和体内对其生物活性进行了测试。与母体药物相比，在大鼠和人肝细胞中三磷酸核苷酸的形成可增加10至20倍。
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