Novel non-nucleoside human cytomegalovirus inhibitors based upon TSAO nucleoside derivatives: structure-activity relationships

Nucleosides Nucleotides Nucleic Acids. 2007;26(6-7):625-8. doi: 10.1080/15257770701490431.


TSAO derivatives are a unique group of potent and highly specific inhibitors of HIV-1 replication. We have recently reported 4''-ureido TSAO derivatives that are devoid of anti-HIV-1 activity, but inhibit human cytomegalovirus with an activity comparable to that of Ganciclovir. We herein report the synthesis and biological evaluation of novel 4''-ureido TSAO derivatives in order to evaluate the structural features required for anti-HCMV activity. Interestingly, these studies revealed that the compounds may inhibit HCMV at the DNA polymerase step via a non-nucleoside mechanism.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology
  • Cytomegalovirus / drug effects*
  • Cytomegalovirus / physiology
  • Humans
  • Nucleosides / pharmacology*
  • Spiro Compounds / chemistry*
  • Spiro Compounds / pharmacology*
  • Structure-Activity Relationship
  • Virus Replication / drug effects


  • Antiviral Agents
  • Nucleosides
  • Spiro Compounds