Truncated phosphonated C-1鈥?branched N,O-nucleosides: A new class of antiviral agents

详细信息	查看全文 | 推荐本文 |

• 作者：Roberto Romeo^a ; ^{robromeo@unime.it} ; Caterina Carnovale^a ; Salvatore V. Giofrè ; ^a ; Giovanni Romeo^a ; Beatrice Macchi^b ; Caterina Frezza^b ; Francesca Marino-Merlo^c ; Venerando Pistarà ; ^d ; Ugo Chiacchio^d
• 关键词：NIEDOPHUBOMIFN-SWLSCSKDSA-N ; UEXXURVZGRXJOJ-WCQYABFASA-N ; JCFRSYGMOISMCD-XHDPSFHLSA-N ; XBYXEFDGSKQWJB-SWLSCSKDSA-N ; LRDTWQCXMAMFPR-WMLDXEAASA-N ; FQURDXJBCRNEAG-UHFFFAOYSA-N ; RWIGWWBLTJLKMK-UHFFFAOYSA-N ; CFXHICSKKKWNKL-UHFFFAOYSA-N ; TULKOCNCHGRRHX-UHFFFAOY
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：1 June, 2012
• 卷：20
• 期：11
• 页码：3652-3657
• 文件大小：703 K

摘要

Truncated phosphonated C-1鈥?branched N,O-nucleosides have been synthesized in good yields by 1,3-dipolar cycloaddition methodology, starting from N-methyl-C-(diethoxyphosphoryl)nitrone 7. Preliminary biological assays show that 尾-anomers are able to inhibit HIV in vitro infection at concentrations in the micromolar range. Higher SI values with respect to AZT indicated that the compounds were endowed with low cytotoxicity.