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Stereoselective Synthesis and Biological Evaluations of Novel 3′-Deoxy-4′-azaribonucleosides as Inhibitors of Hepatitis C Virus RNA Replication

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journal contribution
posted 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
3′-Deoxy-4′-azaribonucleosides (15ad) 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.