Synthesis and Anticonvulsant Activity of Novel Bicyclic Acidic Amino Acids
Journal of Medicinal Chemistry2003Vol. 46(14), pp. 3102–3108
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Paola Conti, Marco De Amici, Samuele Joppolo di Ventimiglia, Tine B. Stensbøl, Ulf Madsen, Hans Bräuner‐Osborne, Emilio Russo, Giovambattista De Sarro, Giuseppe Brunò, Carlo De Micheli
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.
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