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Synthesis and biological activity of glutamic acid derivatives
J M Receveur1, J Guiramand, M Récasens
1Laboratoire des Aminoacides, Peptides et Protéines ESA CNRS 5075, Université Montpellier I & II, France.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
Abstract:
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.