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.
Chiacchio, U., Borrello, L., Crispino, L., Rescifina, A., Merino, P., Macchi, B., et al. (2009). Stereoselective Synthesis and Biological Evaluations of Novel 3 '-Deoxy-4 '-azaribonucleosides as Inhibitors of Hepatitis C Virus RNA Replication. JOURNAL OF MEDICINAL CHEMISTRY, 52(13), 4054-4057 [10.1021/jm900197j].
Stereoselective Synthesis and Biological Evaluations of Novel 3 '-Deoxy-4 '-azaribonucleosides as Inhibitors of Hepatitis C Virus RNA Replication
MACCHI, BEATRICE;BALESTRIERI, EMANUELA;
2009-01-01
Abstract
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.| File | Dimensione | Formato | |
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azaribose nucleosides as potent HCV RdRp inhibitors JMC 2009 ASAP.pdf
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