Synthesis and pharmacological evaluation of. gamma.-aminobutyric acid analogs. New ligand for GABAB sites

P Berthelot, C Vaccher, A Musadad…

Index: Berthelot; Vaccher; Musadad; Flouquet; Debaert; Luyckx Journal of Medicinal Chemistry, 1987 ,  vol. 30,  # 4  p. 743 - 746

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Citation Number: 53

Abstract

Baclofen (0-p-chlorophenyl-GABA) is the only selective agonist for the bicuculline- insensitive GABAB receptor. We report the synthesis of new GABA analogues and baclofen analogues. In vitro, two compounds, 4-amino-3-benzo [b] furan-2-ylbutanoic acid (9g) and 4- amino-3-(5-methoxybenzo [blfuran-2-y1) butanoic acid (9h), showed an affinity for the GABAB receptor. The results obtained with racemic compounds of benzofuran structure, ...