Novel malonamide derivatives as potent kappa opioid receptor agonists

Bioorg Med Chem Lett. 2007 Apr 1;17(7):1951-5. doi: 10.1016/j.bmcl.2007.01.053. Epub 2007 Jan 25.

Abstract

A novel series of malonamide derivatives was synthesized. These amides were shown to be potent and selective kappa opioid receptor agonists.

MeSH terms

  • Chemistry, Pharmaceutical / methods*
  • Cytochrome P-450 CYP2D6 / chemistry
  • Drug Design
  • Drug Evaluation, Preclinical
  • Humans
  • Inhibitory Concentration 50
  • Kinetics
  • Malonates / chemical synthesis*
  • Malonates / chemistry
  • Malonates / pharmacology*
  • Models, Chemical
  • Molecular Conformation
  • Receptors, Opioid, kappa / antagonists & inhibitors*

Substances

  • Malonates
  • Receptors, Opioid, kappa
  • Cytochrome P-450 CYP2D6
  • malonamide