title: Synthesis and biological activity of glutamic acid derivatives.
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.
authors.affiliation: Laboratoire des Aminoacides, Peptides et Protéines ESA CNRS 5075, Université Montpellier I & II, France.
authors.forename: J M
authors.initials: JM
authors.lastname: Receveur
authors.forename: J
authors.initials: J
authors.lastname: Guiramand
authors.forename: M
authors.initials: M
authors.lastname: Récasens
authors.forename: M L
authors.initials: ML
authors.lastname: Roumestant
authors.forename: P
authors.initials: P
authors.lastname: Viallefont
authors.forename: J
authors.initials: J
authors.lastname: Martinez
mesh_terms: D000818:Animals; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D018698:Glutamic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D016548:Prosencephalon / Q000166:cytology / Q000187:drug effects; D051381:Rats; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*; D013574:Synaptosomes / Q000187:drug effects
chemical_list: D018691:Excitatory Amino Acid Antagonists; D018094:Receptors, Metabotropic Glutamate; D018698:Glutamic Acid