Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 11: structural modulations of diaryltriazines with potent anti-HIV activity

Eur J Med Chem. 2008 Jun;43(6):1230-6. doi: 10.1016/j.ejmech.2007.08.001. Epub 2007 Aug 11.


A series of novel 6-naphthyloxy substituted DATA analogues bearing different substituents on the C-6 position of triazine ring were synthesized and evaluated for their in vitro anti-HIV activity in MT-4 cells. The results demonstrated that most of the compounds in this series are potent activity against HIV-1 with moderate to high selectivity. Among these analogues, two compounds exhibited excellent effect in inhibiting HIV-1 replication at nanomolar concentration (for compound 9h: IC(50)=9.3 nM, SI=15,385; for compound 9i: IC(50)=9.4 nM, SI=14,094), which are about 15-fold more active than nevirapine. In addition, several compounds are active against both HIV-1 and HIV-2, whose mechanism may be different from typical NNRTIs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology*
  • Cell Line
  • HIV Reverse Transcriptase / antagonists & inhibitors*
  • HIV-1 / drug effects
  • Humans
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Quantitative Structure-Activity Relationship
  • Reverse Transcriptase Inhibitors / chemistry
  • Reverse Transcriptase Inhibitors / pharmacology*
  • Spectrometry, Mass, Electrospray Ionization
  • Triazines / chemistry
  • Triazines / pharmacology*


  • Anti-HIV Agents
  • Reverse Transcriptase Inhibitors
  • Triazines
  • reverse transcriptase, Human immunodeficiency virus 1
  • HIV Reverse Transcriptase