@article{6910d2bc6feb45ab93b4471fffcad7a8,
title = "Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids",
abstract = "Bicyclic acidic amino acids (+/-)-6 and (+/-)-7, which are conformationally constrained homologues of glutamic acid, were prepared via a strategy based on a 1,3-dipolar cycloaddition. The new amino acids were tested toward ionotropic and metabotropic glutamate receptor subtypes; both of them behaved as antagonists at mGluR1,5 and as agonists at mGluR2. Furthermore, whereas (+/-)-6 was inactive at all ionotropic glutamate receptors, (+/-)-7 displayed a quite potent antagonism at the NMDA receptors. In the in vivo tests on DBA/2 mice, the compounds displayed an anticonvulsant activity. The interesting pharmacological profile of (+/-)-7 qualifies it as a lead of novel neuroprotective agents.",
keywords = "Amino Acids, Acidic, Amino Acids, Dicarboxylic, Animals, Anticonvulsants, CHO Cells, Cerebral Cortex, Cricetinae, Crystallography, X-Ray, Dicarboxylic Acids, Excitatory Amino Acid Agonists, Excitatory Amino Acid Antagonists, Heterocyclic Compounds, 2-Ring, Isoxazoles, Male, Mice, Mice, Inbred DBA, Molecular Conformation, Rats, Receptors, Metabotropic Glutamate, Receptors, N-Methyl-D-Aspartate, Stereoisomerism",
author = "Paola Conti and {De Amici}, Marco and {Joppolo Di Ventimiglia}, Samuele and Stensb{\o}l, {Tine B} and Ulf Madsen and Hans Br{\"a}uner-Osborne and Emilio Russo and {De Sarro}, Giovambattista and Giuseppe Bruno and {De Micheli}, Carlo",
year = "2003",
month = jul,
day = "3",
doi = "10.1021/jm0308085",
language = "English",
volume = "46",
pages = "3102--8",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "14",
}