| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1397642 | European Journal of Medicinal Chemistry | 2011 | 7 Pages |
The synthesis of four new isoxazoline-based amino acids being analogues of previously described glutamate receptor ligands is reported and their affinity for ionotropic glutamate receptors is analyzed in comparison with that of selected model compounds. Molecular modelling investigations have been carried out to rationalize the interaction with the NMDA receptors.
Graphical abstractNew isoxazoline-based acidic amino acids have been synthesized and tested at ionotropic glutamate receptors. Molecular modelling investigations have been carried out to rationalize the interaction with the NMDA receptors.Figure optionsDownload full-size imageDownload as PowerPoint slideResearch highlights► Glutamic acid is the main excitatory neurotransmitter in the CNS. ► NMDA receptors are potential therapeutic targets for treatment of CNS disorders. ► New competitive NMDA receptor antagonists have been synthesized and tested. ► The mode of interaction with NMDA/NR2A subunit has been proposed.
