Synthesis and Antiviral Activity of 2'(β)-Hydroxymethylated Carbodine Analogues Against Hepatitis C Virus

다국어 초록 (Multilingual Abstract)

2'(β)-Hydroxymethylated adenosine is a potent and selective inhibitor of hepatitis C virus (HCV) replication. It
targets the RNA-dependent RNA polymerase of HCV, NS5B. Synthesis and antiviral evaluation of carbocyclic versions
are described. The cyclopentene intermediate (9β) was successfully synthesized through sequential Johnson-Claisen
orthoester rearrangement and ring-closing metathesis (RCM). Coupling of bases via a Pd(0) catalyst, selective dihydroxylation,
and desilylation yielded the target nucleoside analogues. The compounds 17 and 18 were assayed for their
ability to inhibit HCV RNA replication in a subgenomic replicon Huh7 cell line and showed moderate antiviral activity
with toxicity up to 20.0 and 24.7 μg/mL, respectively.

참고문헌 (Reference)

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