Stereospecific synthesis and antiviral properties of different enantiomerically pure carbocyclic 2'-deoxyribonucleoside analogues derived from common chiral pools: (+)-(1R,5S)- and (-)-(1S,5R)-2-oxabicyclo[3.3.0]oct-6-en-3-one

J Med Chem. 1990 May;33(5):1353-60. doi: 10.1021/jm00167a011.

Abstract

Enantiomerically pure (+)- and (-)-carbocyclic thymidine, (-)-carbocyclic 3'-epi-thymidine, (+)-carbocyclic 3'-deoxy-3'-azidothymidine, (+)-carbocyclic 2,3'-O-anhydrothymidine, (+)-carbocyclic 3'-O,6'-methylenethymidine, and (+)-(6'S)-carbocyclic 6'-methylthymidine were synthesized in a stereospecific manner from common chiral pools of (+)-(1R,5S)- and (-)-(1S,5R)-2-oxabicyclo[3.3.0]oct-6-en-3-one and evaluated for antiviral activity. (+)-Carbathymidine and, to a lesser extent, (+)-carbocyclic 2'-deoxyadenosine proved to be effective against HSV-1 [minimum inhibitory concentration (MIC): 0.2 and 2 micrograms/mL, respectively] and HSV-2 (MIC: 2 and 20 micrograms/mL, respectively), but virtually inactive against TK- HSV-1 (MIC: 40 and 100 micrograms/mL, respectively). (+)-Carbathymidine was also active against vaccinia virus (2 micrograms/mL). None of the compounds had a specific effect on the replication of HIV or other RNA viruses.

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Bridged Bicyclo Compounds / chemical synthesis*
  • Bridged-Ring Compounds / chemical synthesis*
  • Chemical Phenomena
  • Chemistry
  • Microbial Sensitivity Tests
  • Simplexvirus / drug effects
  • Stereoisomerism
  • Structure-Activity Relationship
  • Thymidine / analogs & derivatives*
  • Thymidine / chemical synthesis
  • Thymidine / pharmacology
  • Vaccinia virus / drug effects

Substances

  • Antiviral Agents
  • Bridged Bicyclo Compounds
  • Bridged-Ring Compounds
  • carbathymidine
  • Thymidine