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Stereoselective Synthesis And Biological Evaluations Of Novel 3'-deoxy-4'-azaribonucleosides As Inhibitors Of Hepatitis C Virus RNA Replication.

U. Chiacchio, L. Borrello, Lia Crispino, A. Rescifina, P. Merino, B. Macchi, E. Balestrieri, A. Mastino, A. Piperno, G. Romeo
Published 2009 · Chemistry, Medicine

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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.
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