Huang Qiuya, Herdewijn Piet
Laboratory of Medicinal Chemistry, Rega Institute for Medical Research, K.U. Leuven, Leuven, Belgium.
Nucleosides Nucleotides Nucleic Acids. 2009 May;28(5):337-51. doi: 10.1080/15257770903044184.
The synthesis and antiviral evaluation of new 3'-O-phosphonoethyl modified phosphonate nucleosides related to PMDTA and PMDTT is described. The reaction scheme starts from protected L-threose and the phosphonate group is introduced by the Arbuzov reaction. The 2'-OH as well as the 2'-deoxygenated nucleosides have been obtained. Unfortunately, none of these synthesized compounds shows activity against HIV and HCV.
描述了与PMDTA和PMDTT相关的新型3'-O-膦酰基乙基修饰的膦酸酯核苷的合成及抗病毒评估。反应方案从受保护的L-苏糖开始,膦酸酯基团通过阿尔布佐夫反应引入。已获得2'-OH以及2'-脱氧核苷。遗憾的是,这些合成化合物均未显示出对HIV和HCV的活性。