6-Benzylamino 4-oxo-1,4-dihydro-1,8-naphthyridines and 4-oxo-1,4-dihydroquinolines as HIV integrase inhibitors

Bioorg Med Chem Lett. 2011 Jan 15;21(2):760-3. doi: 10.1016/j.bmcl.2010.11.108. Epub 2010 Nov 30.

Abstract

SAR studies on the quinolone carboxylic acid class of HIV-1 integrase inhibitors focused on improving the metabolic stability and led to the discovery of 27 and 38.

MeSH terms

  • Animals
  • Dogs
  • HIV Infections / drug therapy
  • HIV Integrase Inhibitors / chemistry
  • HIV Integrase Inhibitors / metabolism*
  • HIV Integrase Inhibitors / pharmacokinetics
  • HIV Integrase Inhibitors / pharmacology*
  • HIV-1 / enzymology*
  • Haplorhini
  • Humans
  • Microsomes, Liver / metabolism*
  • Naphthyridines / chemistry
  • Naphthyridines / metabolism
  • Naphthyridines / pharmacokinetics
  • Naphthyridines / pharmacology
  • Quinolines / chemistry
  • Quinolines / metabolism*
  • Quinolines / pharmacokinetics
  • Quinolines / pharmacology*
  • Rats
  • Structure-Activity Relationship

Substances

  • 1,4-dihydroquinoline
  • HIV Integrase Inhibitors
  • Naphthyridines
  • Quinolines