Regioisomeric 3-carboxyisoxazolinyl prolines (CIP-A and CIP-B) and 3-hydroxyisoxazolinyl prolines [(±)-8 and (±)-9] were synthesized and assayed for glutamate receptor activity. CIP-A [(±)-6] showed a convulsant activity evaluated in vivo on DBA/2 mice, higher than AMPA and similar to kainic acid. The eutomer of CIP-A [CIP-AS, (-)-6], obtained from (S)-3,4-didehydroproline, evidenced common stereochemical requirements with AMPA and kainic acid. Copyright (C) 2000 Elsevier Science S.A.
Design of new analogues of glutamic acid with a conformationally restricted structure / P. Conti, M. De Amici, C. De Micheli. - In: IL FARMACO. - ISSN 0014-827X. - 55:3(2000), pp. 162-164.
Design of new analogues of glutamic acid with a conformationally restricted structure
P. ContiPrimo
;M. De AmiciSecondo
;C. De MicheliUltimo
2000
Abstract
Regioisomeric 3-carboxyisoxazolinyl prolines (CIP-A and CIP-B) and 3-hydroxyisoxazolinyl prolines [(±)-8 and (±)-9] were synthesized and assayed for glutamate receptor activity. CIP-A [(±)-6] showed a convulsant activity evaluated in vivo on DBA/2 mice, higher than AMPA and similar to kainic acid. The eutomer of CIP-A [CIP-AS, (-)-6], obtained from (S)-3,4-didehydroproline, evidenced common stereochemical requirements with AMPA and kainic acid. Copyright (C) 2000 Elsevier Science S.A.
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