Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase--structure-activity relationships and crystallographic analysis

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1131-4. doi: 10.1016/j.bmcl.2007.11.127. Epub 2007 Dec 5.

Abstract

A series of 3,4,5-trisubstituted 1,2,4-4H triazole derivatives was synthesized and investigated for HIV-1 reverse transcriptase inhibition. An X-ray structure with HIV-1 RT secured the binding mode and allowed the key interactions with the enzyme to be identified.

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology*
  • Combinatorial Chemistry Techniques
  • Crystallography, X-Ray
  • HIV Reverse Transcriptase / antagonists & inhibitors*
  • HIV-1 / drug effects*
  • Molecular Conformation
  • Molecular Structure
  • Reverse Transcriptase Inhibitors / chemical synthesis*
  • Reverse Transcriptase Inhibitors / chemistry
  • Reverse Transcriptase Inhibitors / pharmacology*
  • Structure-Activity Relationship
  • Triazoles / chemical synthesis*
  • Triazoles / chemistry
  • Triazoles / pharmacology*

Substances

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