Synthesis of new isoxazoline-based acidic amino acids and investigation of their affinity and selectivity profile at ionotropic glutamate receptors
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 c...
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Published in | European journal of medicinal chemistry Vol. 46; no. 2; pp. 787 - 793 |
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Main Authors | , , , , , , |
Format | Journal Article |
Language | English |
Published |
ISSY-LES-MOULINEAUX
Elsevier Masson SAS
01.02.2011
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | 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.
New 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.
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► 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. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0223-5234 1768-3254 |
DOI: | 10.1016/j.ejmech.2010.12.020 |