New oxapolycyclic cage amines with NMDA receptor antagonist and trypanocidal activities

Bioorg Med Chem. 2010 Jan 1;18(1):46-57. doi: 10.1016/j.bmc.2009.11.017. Epub 2009 Nov 14.

Abstract

The synthesis of several (1,2,3,5,6,7-hexahydro-1,5:3,7-dimethano-4-benzoxonin-3-yl)amines and related compounds is reported. Several of them display very similar activity to memantine as NMDA receptor antagonists. Several derivatives showed a significant level of trypanocidal activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemical synthesis
  • Amines / chemistry*
  • Amines / pharmacology*
  • Animals
  • Antiparkinson Agents / chemical synthesis
  • Antiparkinson Agents / chemistry
  • Antiparkinson Agents / pharmacology
  • Cells, Cultured
  • Humans
  • Memantine / pharmacology
  • Molecular Structure
  • Neurons / drug effects
  • Parkinson Disease / drug therapy
  • Rats
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
  • Receptors, N-Methyl-D-Aspartate / metabolism
  • Trypanocidal Agents / chemical synthesis
  • Trypanocidal Agents / chemistry*
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma brucei brucei / drug effects
  • Trypanosomiasis / drug therapy

Substances

  • Amines
  • Antiparkinson Agents
  • Receptors, N-Methyl-D-Aspartate
  • Trypanocidal Agents
  • Memantine