Griffon Jean-Francois, Dumas Audrey, Storer Richard, Sommadossi Jean-Pierre, Gosselin Gilles
Idenix Pharmaceuticals, Medicinal Chemistry Laboratory, Montpellier, France.
Nucleosides Nucleotides Nucleic Acids. 2009 May;28(5):435-49. doi: 10.1080/15257770903044531.
In the search for inhibitors of the replication of RNA viruses, including hepatitis C virus (HCV), the hitherto unknown 4'-C-azidomethyl-beta-D-ribofuranosyl nucleosides of the five naturally occurring nucleic acid bases have been synthesized and their antiviral properties examined. These 4'-C-branched nucleosides were stereospecifically prepared by glycosylation of purine and pyrimidine aglycons with a suitable peracylated 4-C-azidomethyl-D-pentofuranose sugar, followed by removal of the protecting groups. The prepared compounds were tested for their activity against several viruses, but they did not show an antiviral effect.
在寻找包括丙型肝炎病毒(HCV)在内的RNA病毒复制抑制剂的过程中,已合成了五种天然存在的核酸碱基的迄今未知的4'-C-叠氮甲基-β-D-呋喃核糖核苷,并对其抗病毒特性进行了研究。这些4'-C-支链核苷是通过嘌呤和嘧啶苷元与合适的全酰化4-C-叠氮甲基-D-戊呋喃糖进行糖基化反应,然后除去保护基团而立体定向制备的。对所制备的化合物进行了几种病毒的活性测试,但它们未显示出抗病毒作用。