Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: Design, synthesis, and pharmacological characterization
Research output: Contribution to journal › Journal article › Research › peer-review
The design and synthesis of new N1-substituted 3-carboxy- and 3-phosphonopyrazoline and pyrazole amino acids that target the glutamate binding site of NMDA receptors are described. An analysis of the stereochemical requirements for high-affinity interaction with these receptors was performed. We identified two highly potent and selective competitive NMDA receptor antagonists, (5S,alphaR)-1 and (5S,alphaR)-4, which exhibit good in vitro neuroprotective activity and in vivo anticonvulsant activity by i.p. administration, suggesting that these molecules may have potential use as therapeutic agents.
Original language | English |
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Journal | ChemMedChem |
Volume | 5 |
Issue number | 9 |
Pages (from-to) | 1465-1475 |
ISSN | 1860-7179 |
DOIs | |
Publication status | Published - 2010 |
- Former Faculty of Pharmaceutical Sciences
Research areas
ID: 21699538