Phosphoramidate protides of 2',3'-dideoxy-3'-fluoroadenosine and related nucleosides with potent activity against HIV and HBV |
| |
| Authors: | Gudmundsson Kristjan S Daluge Susan M Johnson Lance C Jansen Robert Hazen Richard Condreay Lynn D McGuigan Christopher |
| |
| Affiliation: | Division of Chemistry, GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA. Kristjan.S.Gudmundsson@gsk.com |
| |
| Abstract: | Syntheses of phosphoramidate protides of several 2',3'-dideoxy-3'-fluoroadenosine derivatives by treatment of the nucleoside with phosphorochloridates in the presence of pyridine and t-BuMgCl is described. Several of these protides showed significantly improved antiviral potency over the parent nucleoside against HIV and HBV. Especially marked was the improvement in potency of phosphoramidate protides of 2',3'-dideoxy-3'-fluoroadenosine against both HIV and HBV. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
