Phosphonated carbocyclic 2'-oxa-3'-azanucleosides as new antiretroviral agents

J Med Chem. 2007 Jul 26;50(15):3747-50. doi: 10.1021/jm070285r. Epub 2007 Jun 20.

Abstract

Phosphonated carbocyclic 2'-oxa-3'-azanucleosides have been synthesized and tested for their antiretroviral activity. The obtained results have shown that some of the compounds were as powerful as azydothymidine in inhibiting the reverse transcriptase activity of the human retrovirus T-cell leukemia/lymphotropic virus type 1 and in protecting human peripheral blood mononuclear cells against human retrovirus T-cell leukemia/lymphotropic virus type 1 transmission in vitro. These data indicate that phosphonated carbocyclic 2'-oxa-3'-azanucleosides possess the necessary requirements to efficiently counteract infections caused by human retroviruses.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Retroviral Agents / chemical synthesis*
  • Anti-Retroviral Agents / chemistry
  • Anti-Retroviral Agents / pharmacology
  • Aza Compounds / chemical synthesis*
  • Aza Compounds / chemistry
  • Aza Compounds / pharmacology
  • Human T-lymphotropic virus 1 / drug effects*
  • Human T-lymphotropic virus 1 / enzymology
  • Human T-lymphotropic virus 1 / pathogenicity
  • Humans
  • In Vitro Techniques
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / virology
  • Organophosphonates / chemical synthesis*
  • Organophosphonates / chemistry
  • Organophosphonates / pharmacology
  • Purine Nucleosides / chemical synthesis*
  • Purine Nucleosides / chemistry
  • Purine Nucleosides / pharmacology
  • Pyrimidine Nucleosides / chemical synthesis*
  • Pyrimidine Nucleosides / chemistry
  • Pyrimidine Nucleosides / pharmacology
  • Reverse Transcriptase Inhibitors / chemical synthesis
  • Reverse Transcriptase Inhibitors / chemistry
  • Reverse Transcriptase Inhibitors / pharmacology
  • Structure-Activity Relationship

Substances

  • Anti-Retroviral Agents
  • Aza Compounds
  • Organophosphonates
  • Purine Nucleosides
  • Pyrimidine Nucleosides
  • Reverse Transcriptase Inhibitors