Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors

Bioorg Med Chem. 2008 Aug 1;16(15):7429-35. doi: 10.1016/j.bmc.2008.06.012. Epub 2008 Jun 13.


Several N(1)-substituted 1,3-dihydro-2H-benzimidazol-2-ones were synthesized and evaluated as anti-HIV agents. Some of them proved to be highly effective in inhibiting HIV-1 replication at nanomolar concentration as potent non-nucleoside HIV-1 RT inhibitors (NNRTIs) with low cytotoxicity. SAR studies highlighted that the nature of the substituents at N(1) and on the benzene ring of benzimidazolone moiety significantly influenced the anti-HIV activity of this class of potent antiretroviral agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Benzimidazoles / chemistry*
  • Benzimidazoles / pharmacology*
  • Cell Line
  • HIV-1 / drug effects
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Reverse Transcriptase Inhibitors / chemistry*
  • Reverse Transcriptase Inhibitors / pharmacology*
  • Structure-Activity Relationship
  • Virus Replication


  • Anti-HIV Agents
  • Benzimidazoles
  • Reverse Transcriptase Inhibitors