A potent and orally active HIV-1 integrase inhibitor

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1392-8. doi: 10.1016/j.bmcl.2006.11.080. Epub 2006 Dec 3.

Abstract

A 1,6-naphthyridine inhibitor of HIV-1 integrase has been discovered with excellent inhibitory activity in cells, good pharmacokinetics, and an excellent ability to inhibit virus with mutant enzyme.

MeSH terms

  • Administration, Oral
  • Animals
  • Cells, Cultured
  • HIV Integrase / drug effects
  • HIV Integrase / genetics
  • HIV Integrase Inhibitors / chemical synthesis*
  • HIV Integrase Inhibitors / pharmacokinetics*
  • HIV Integrase Inhibitors / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Mutation
  • Naphthyridines / chemical synthesis*
  • Naphthyridines / pharmacokinetics
  • Naphthyridines / pharmacology
  • Rats
  • Structure-Activity Relationship

Substances

  • HIV Integrase Inhibitors
  • Naphthyridines
  • HIV Integrase