Stereoselective Synthesis and Biological Evaluations of Novel 3′-Deoxy-4′-azaribonucleosides as Inhibitors of Hepatitis C Virus RNA Replication
journal contributionposted on 09.07.2009 by Ugo Chiacchio, Luisa Borrello, Lia Crispino, Antonio Rescifina, Pedro Merino, Beatrice Macchi, Emanuela Balestrieri, Antonio Mastino, Anna Piperno, Giovanni Romeo
Any type of content formally published in an academic journal, usually following a peer-review process.
3′-Deoxy-4′-azaribonucleosides (15a−d) were synthesized starting from the commercially available (4R)-trans-4-hydroxy-l-proline 7. From biological evaluations, 15b and 15d emerged as potent inhibitors of HCV replication on a replicon assay. These findings demonstrate that synthesized pyrrolidine nucleosides represent a new template for antiviral or other biological studies and could be considered for novel combination therapy against HCV infection using nucleoside inhibitors and non-nucleoside inhibitors of HCV NS5B.