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Synthesis and biological activity of glutamic acid derivatives.

Authors
  • Receveur, J M
  • Guiramand, J
  • Récasens, M
  • Roumestant, M L
  • Viallefont, P
  • Martinez, J
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Jan 20, 1998
Volume
8
Issue
2
Pages
127–132
Identifiers
PMID: 9871639
Source
Medline
License
Unknown

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.

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