Synthesis of novel N1-substituted bicyclic pyrazole amino acids and evaluation of their interaction with glutamate receptors

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N1-substituted bicyclic pyrazole amino acids (S)-9a-9c and (R)-9a-9c, which are conformationally constrained analogues of glutamic acid, were prepared via a strategy based on a 1,3-dipolar cycloaddition. The new amino acids were tested for activity at ionotropic and metabotropic glutamate receptors. Some of them turned out to be selective for the NMDA receptors, where they behaved as weak antagonists. The biological activity is mainly due to the interaction with the glutamate binding site, and not with the glycine co-agonist site.
Original languageEnglish
JournalChemistry & Biodiversity
Issue number6
Pages (from-to)748-57
Publication statusPublished - Jun 2005

    Research areas

  • Bicyclo Compounds, Heterocyclic, Excitatory Amino Acid Agonists, Excitatory Amino Acid Antagonists, Molecular Structure, Receptors, Glutamate

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