Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents

Bioorg Med Chem. 2009 Aug 15;17(16):5962-7. doi: 10.1016/j.bmc.2009.06.068. Epub 2009 Jul 3.


Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have become very important components in the antiretroviral combination therapies used to treat HIV. Recently, our group identified some 1,3-dihydrobenzimidazol-2-one derivatives and their sulfones as a potent and novel class of NNRTIs. We herein report the synthesis and biological evaluation of the new compounds in which different structural modifications have been introduced in order to investigate their effects on RT inhibition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Benzimidazoles / chemical synthesis
  • Benzimidazoles / chemistry*
  • Benzimidazoles / pharmacology
  • Cell Line
  • Drug Design
  • HIV Reverse Transcriptase / antagonists & inhibitors*
  • HIV Reverse Transcriptase / metabolism
  • Humans
  • Reverse Transcriptase Inhibitors / chemical synthesis*
  • Reverse Transcriptase Inhibitors / chemistry
  • Reverse Transcriptase Inhibitors / pharmacology
  • Structure-Activity Relationship


  • Anti-HIV Agents
  • Benzimidazoles
  • Reverse Transcriptase Inhibitors
  • benzimidazolone
  • HIV Reverse Transcriptase