Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists

Bioorg Med Chem Lett. 2006 Feb;16(3):681-5. doi: 10.1016/j.bmcl.2005.10.028. Epub 2005 Nov 2.

Abstract

Synthesis, SAR, and binding affinities are described for a new class of 1,8-naphthyridinone CB1 receptor specific inverse agonists. Food intake, knockout mouse, and pharmacokinetic evaluation of 14 indicate that this compound is an effective orally active modulator of CB1.

Publication types

  • Evaluation Study

MeSH terms

  • Administration, Oral
  • Animals
  • Binding Sites
  • Eating / drug effects*
  • Mice
  • Mice, Knockout
  • Models, Chemical
  • Naphthyridines / chemical synthesis
  • Receptor, Cannabinoid, CB1 / agonists
  • Receptor, Cannabinoid, CB1 / antagonists & inhibitors*

Substances

  • Naphthyridines
  • Receptor, Cannabinoid, CB1