9-(2-β-C-甲基-β-D-呋喃核糖基)-6-取代嘌呤衍生物作为丙型肝炎病毒RNA复制抑制剂的合成
Synthesis of 9-(2-beta-C-methyl-beta-d-ribofuranosyl)-6-substituted purine derivatives as inhibitors of HCV RNA replication.
作者信息
Ding Yili, Girardet Jean-Luc, Hong Zhi, Lai Vicky C H, An Haoyun, Koh Yung-Hyo, Shaw Stephanie Z, Zhong Weidong
机构信息
Valeant Pharmaceuticals International, 3300 Hyland Avenue Costa Mesa, CA 92626, USA.
出版信息
Bioorg Med Chem Lett. 2005 Feb 1;15(3):709-13. doi: 10.1016/j.bmcl.2004.11.020.
A series of 9-(2'-beta-C-methyl-beta-d-ribofuranosyl)-6-substituted purine derivatives were synthesized as potential inhibitors of HCV RNA replication. Their inhibitory activities in a cell based HCV replicon assay were reported. A prodrug approach was used to further improve the potency of these compounds by increasing the intracellular levels of 5'-monophosphate metabolites. These nucleotide prodrugs showed much improved inhibitory activities of HCV RNA replication.
合成了一系列9-(2'-β-C-甲基-β-D-呋喃核糖基)-6-取代嘌呤衍生物，作为潜在的丙型肝炎病毒(HCV)RNA复制抑制剂。报道了它们在基于细胞的HCV复制子试验中的抑制活性。采用前药方法，通过提高5'-单磷酸代谢物的细胞内水平来进一步提高这些化合物的效力。这些核苷酸前药显示出对HCV RNA复制的抑制活性有显著改善。
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