Novel benzopolycyclic amines with NMDA receptor antagonist activity

Bioorg Med Chem. 2014 May 1;22(9):2678-83. doi: 10.1016/j.bmc.2014.03.025. Epub 2014 Mar 24.

Abstract

A new series of benzopolycyclic amines active as NMDA receptor antagonists were synthesized. Most of them exhibited increased activity compared with related analogues previously published. All the tested compounds were more potent than clinically approved amantadine and one of them displayed a lower IC50 value than memantine, an anti-Alzheimer's approved drug.

Keywords: Amantadine; Memantine; NMDA; Polycyclic compounds; Prins–Ritter reaction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amantadine / chemistry
  • Amantadine / metabolism
  • Amines / chemical synthesis
  • Amines / chemistry*
  • Amines / metabolism
  • Memantine / chemistry
  • Memantine / metabolism
  • Neuroprotective Agents / chemical synthesis
  • Neuroprotective Agents / chemistry
  • Neuroprotective Agents / metabolism
  • Protein Binding
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
  • Receptors, N-Methyl-D-Aspartate / metabolism

Substances

  • Amines
  • Neuroprotective Agents
  • Receptors, N-Methyl-D-Aspartate
  • Amantadine
  • Memantine