3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates--a new class of HIV-1 integrase inhibitors

Bioorg Med Chem Lett. 2009 Apr 1;19(7):1930-4. doi: 10.1016/j.bmcl.2009.02.055. Epub 2009 Feb 20.

Abstract

A new class of inhibitors of HIV-1 integrase has been optimized to provide selective and highly efficient strand transfer inhibition.

MeSH terms

  • Animals
  • HIV Integrase / metabolism*
  • HIV Integrase Inhibitors / chemical synthesis*
  • HIV Integrase Inhibitors / chemistry
  • HIV Integrase Inhibitors / pharmacokinetics
  • HIV-1 / drug effects
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacokinetics
  • Rats
  • Structure-Activity Relationship

Substances

  • HIV Integrase Inhibitors
  • Pyrimidines
  • HIV Integrase
  • p31 integrase protein, Human immunodeficiency virus 1