Pyrazole NNRTIs 1: design and initial optimisation of a novel template

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5599-602. doi: 10.1016/j.bmcl.2009.08.039. Epub 2009 Aug 13.

Abstract

The design and synthesis of a novel series of non-nucleoside HIV reverse transcriptase inhibitors (NNRTIs) based on a pyrazole template is described. These compounds are active against wild type reverse transcriptase (RT) and retain activity against clinically important mutants.

MeSH terms

  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / pharmacology
  • Drug Design
  • HIV Reverse Transcriptase / antagonists & inhibitors*
  • HIV Reverse Transcriptase / metabolism
  • Humans
  • Microsomes, Liver / metabolism
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology
  • Reverse Transcriptase Inhibitors / chemical synthesis
  • Reverse Transcriptase Inhibitors / chemistry*
  • Reverse Transcriptase Inhibitors / pharmacology
  • Structure-Activity Relationship

Substances

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