Synthesis and biological evaluation of 5R- and 5S-methyl substituted D- and L-configuration 1,3-dioxolane nucleoside analogs

Bioorg Med Chem. 2004 Dec 1;12(23):6237-47. doi: 10.1016/j.bmc.2004.08.054.

Abstract

1,3-Dioxolane and 1,3-oxathiolane nucleoside analogs play an important role in anti-viral and anti-neoplastic chemotherapy. We report here the synthesis of 2-hydroxymethyl-5-methyl-1,3-dioxolanylpurine nucleosides from 4-acetoxy-2-(benzyloxymethyl)-5-methyldioxolane. Dioxolanes of alpha-D-, beta-D-, alpha-L-, and beta-L-configuration were prepared, that included 5-methyl derivatives of both 5R and 5S configuration. Molecular mechanics calculations indicate that the 5S and 5R diastereoisomeric 1,3-dioxolanes possess distinct conformational bias, suggesting that methyl substitution may alter the conformational preference of 1,3-dioxolanes. The ability of the 1,3-dioxolanes to inhibit HCV RNA replication was evaluated in a cell-based, subgenomic replicon assay. In addition, activity against vaccinia and HIV was evaluated in cell-based assays. The 2-hydroxymethyl-5-methyl-1,3-dioxolanes were found to be inactive.

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology
  • Dioxolanes / chemical synthesis*
  • Dioxolanes / pharmacology
  • Guanosine / analogs & derivatives*
  • HIV / drug effects
  • Hepacivirus / drug effects
  • Nucleosides / chemical synthesis*
  • Nucleosides / pharmacology
  • RNA, Viral / drug effects
  • Stereoisomerism
  • Structure-Activity Relationship
  • Vaccinia virus / drug effects
  • Virus Replication / drug effects

Substances

  • Antiviral Agents
  • Dioxolanes
  • Nucleosides
  • RNA, Viral
  • dioxolane guanosine
  • Guanosine