Design of new analogues of glutamic acid with a conformationally restricted structure

Authors
Conti, P De Amici, M De Micheli, C
Citation
P. Conti et al., Design of new analogues of glutamic acid with a conformationally restricted structure, FARMACO, 55(3), 2000, pp. 162-164
Citations number
10
Categorie Soggetti
Pharmacology & Toxicology
Journal title
FARMACO
ISSN journal
0014827X → ACNP
Volume
55
Issue
3
Year of publication
2000
Pages
162 - 164
Database
ISI
SICI code
0014-827X(200003)55:3<162:DONAOG>2.0.ZU;2-3
Abstract
Regioisomeric 3-carboxyisoxazolinyl prolines (CIP-A and CIP-B) and 3-hydrox yisoxazolinyl prolines [(+/-)-8 and(+/-)-9] were synthesized and assayed fo r glutamate receptor activity. CIP-A [(+/-)-6] showed a convulsant activity evaluated in vivo on DBA/2 mice, higher than AMPA and similar to kainic ac id. The eutomer of CLP-A [CIP-AS, (-)-6], obtained from (S)-3,4-didehydropr oline, evidenced common stereochemical requirements with AMPA and kainic ac id. (C) 2000 Elsevier Science S.A. All rights reserved.