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- W1938182285 abstract "Background: Ribonucleoside analogs possessing a β-methyl substituent at the 2′-position of the d-ribose moiety have been previously discovered to be potent and selective inhibitors of hepatitis C virus (HCV) replication, their triphosphates acting as alternative substrate inhibitors of the HCV RdRp NS5B. Results/methodology: In this article, the authors detail the synthesis, anti-HCV evaluation in cell-based replicon assays and structure–activity relationships of several phosphoramidate diester derivatives of 2′-C-methylguanosine (2′-MeG). Conclusion: The most promising compound, namely the O-[S-(hydroxyl)pivaloyl-2-thioethyl]{abbreviated as O-[(HO)tBuSATE)]} N-benzylamine phosphoramidate diester derivative (IDX184), was selected for further in vivo studies, and was the first clinical pronucleotide evaluated for the treatment of chronic hepatitis C up to Phase II trials." @default.
- W1938182285 created "2016-06-24" @default.
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- W1938182285 date "2015-09-01" @default.
- W1938182285 modified "2023-10-17" @default.
- W1938182285 title "Design, synthesis and antiviral evaluation of 2′-<i>C</i>-methyl branched guanosine pronucleotides: the discovery of IDX184, a potent liver-targeted HCV polymerase inhibitor" @default.
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