1,2,3-Selenadiazole thioacetanilides: synthesis and anti-HIV activity evaluation

Bioorg Med Chem. 2009 Sep 1;17(17):6374-9. doi: 10.1016/j.bmc.2009.07.027. Epub 2009 Jul 18.


The development of new HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating novel structures of increased potency. Based on the bioisosteric principle, novel series of 1,2,3-selenadiazole thioacetanilide derivatives were designed, and synthesized using an original synthetic route, structurally confirmed by spectral analysis, and evaluated for their anti-HIV activity in MT-4 cells. The results showed that only compound 7f possessed potent activity against HIV-1 replication (EC(50)=2.45 microM) similar to the prototype series of sulfanyltriazoles. None of the compounds were active against HIV-2 replication.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetanilides / chemical synthesis*
  • Acetanilides / chemistry*
  • Acetanilides / pharmacology
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Cell Line
  • HIV-1 / drug effects
  • Humans
  • Reverse Transcriptase Inhibitors / chemical synthesis*
  • Reverse Transcriptase Inhibitors / chemistry
  • Reverse Transcriptase Inhibitors / pharmacology
  • Virus Replication / drug effects


  • 1,2,3-selenadiazole thioacetanilide
  • Acetanilides
  • Anti-HIV Agents
  • Reverse Transcriptase Inhibitors
  • thioacetanilide