Benzoxazinones as potent positive allosteric AMPA receptor modulators: part I

Bioorg Med Chem Lett. 2011 Jul 1;21(13):3923-6. doi: 10.1016/j.bmcl.2011.05.026. Epub 2011 May 14.

Abstract

AMPA receptors (AMPARs) are an increasingly important therapeutic target in the CNS. Aniracetam, the first identified potentiator of AMPARs, led to the rigid and more potent CX614. This lead molecule was optimized in order to increase affinity towards the AMPA receptor. The substitution of the dioxine with a benzoxazinone ring system increased the activity and allowed further investigation of the sidechain SAR.

MeSH terms

  • Allosteric Regulation
  • Animals
  • Benzoxazines / chemistry*
  • Benzoxazines / pharmacology*
  • Molecular Structure
  • Nootropic Agents / pharmacology
  • Prosencephalon / drug effects
  • Pyrrolidinones / chemistry
  • Pyrrolidinones / pharmacology
  • Rats
  • Receptors, AMPA / metabolism*
  • Structure-Activity Relationship

Substances

  • Benzoxazines
  • Nootropic Agents
  • Pyrrolidinones
  • Receptors, AMPA
  • aniracetam