Wang Peiyuan, Hollecker Laurent, Pankiewicz Krzysztof W, Patterson Steven E, Whitaker Tony, McBrayer Tamara R, Tharnish Phillip M, Stuyver Lieven J, Schinazi Raymond F, Otto Michael J, Watanabe Kyoichi A
Department of Chemistry, Pharmasset, Inc., Tucker, GA 30084, USA.
Nucleosides Nucleotides Nucleic Acids. 2005;24(5-7):957-60. doi: 10.1081/ncn-200059314.
We recently discovered a novel compound, identified as N3, 5-cyclo-4-(beta-D-ribofuranosyl)-vic-triazolo[4,5-b]pyridinin-5-one, with anti-hepatitis C virus (HCV) activity in vitro. The structure was confirmed by chemical synthesis from 2-hydroxy-5-nitropyridine. It showed anti-HCV activity with EC50= 19.7 microM in replicon cells. Its 3'-deoxy sugar analogue was also synthesized, but was inactive against HCV in vitro.
我们最近发现了一种新型化合物，鉴定为N3, 5-环-4-(β-D-呋喃核糖基)-vic-三唑并[4,5-b]吡啶-5-酮，在体外具有抗丙型肝炎病毒（HCV）活性。其结构通过由2-羟基-5-硝基吡啶进行化学合成得以证实。它在复制子细胞中表现出抗HCV活性，EC50 = 19.7微摩尔。其3'-脱氧糖类似物也已合成，但在体外对HCV无活性。
