Synthesis and biological activity of glutamic acid derivatives
| Autor: | Jean-Marie Receveur, M. L. Roumestant, Philippe Viallefont, Janique Guiramand, Jean Martinez, Max Récasens |
|---|---|
| Přispěvatelé: | Laboratoire des Amino-acides Peptides et Protéines (LAPP), Centre National de la Recherche Scientifique (CNRS)-Université Montpellier 2 - Sciences et Techniques (UM2)-Université Montpellier 1 (UM1), Neurobiologie de l'audition-plasticité synaptique, Institut National de la Santé et de la Recherche Médicale (INSERM), Institut des Biomolécules Max Mousseron [Pôle Chimie Balard] (IBMM), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-Université de Montpellier (UM)-Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM) |
| Rok vydání: | 1998 |
| Předmět: |
MESH: Rats
Stereochemistry Clinical Biochemistry Glutamic Acid Pharmaceutical Science Receptors Metabotropic Glutamate 010402 general chemistry 01 natural sciences Biochemistry Chemical synthesis MESH: Prosencephalon Prosencephalon Drug Discovery Animals MESH: Animals MESH: Receptors Metabotropic Glutamate Molecular Biology chemistry.chemical_classification 010405 organic chemistry Chemistry Organic Chemistry Glutamate receptor Antagonist Biological activity MESH: Excitatory Amino Acid Antagonists MESH: Glutamic Acid Glutamic acid Rats 0104 chemical sciences 3. Good health Metabotropic receptor Dicarboxylic acid Metabotropic glutamate receptor MESH: Synaptosomes Molecular Medicine [SDV.NEU]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC] Excitatory Amino Acid Antagonists Synaptosomes |
| Zdroj: | Bioorganic and Medicinal Chemistry Letters Bioorganic and Medicinal Chemistry Letters, Elsevier, 1998, 8 (2), pp.127-32. ⟨10.1016/S0960-894X(97)10208-6⟩ |
| ISSN: | 0960-894X |
| Popis: | International audience; In order to develop new specific glutamate analogues at metabotropic glutamate receptors, Diels-Alder, 1-4 ionic and radical reactions were performed starting from (2S)-4-methyleneglutamic acid. Preliminary pharmacological evaluation by measuring IP accumulation using rat forebrain synaptoneurosomes has shown that (2S)-4-(2-phthalimidoethyl)glutamic acid (3a), (2S)-4-(4-phthalimidobutyl)glutamic acid (3b) and 1-[(S)-2-amino-2-carboxyethyl]-3,4-dimethylcyclohex-3-ene-1-carbox ylic acid (8) presented moderate antagonist activities. |
| Databáze: | OpenAIRE |
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