Synthesis, pharmacology and X-ray studies of baclofen analogues

P Berthelot, C Vaccher, N Flouquet, M Luyckx…

Index: Berthelot; Vaccher; Flouquet; Luyckx; Brunet; Boulanger; Frippiat; Vercauteren; Debaert; Evrard; Durant European Journal of Medicinal Chemistry, 1991 , vol. 26, # 4 p. 395 - 402

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Citation Number: 14

Abstract

Abstract Baclofen (β-p-chlorophenyl-GABA) is the reference selective agonist for the bicuculline-insensitive GABA B receptor. The search for new compounds having a high affinity for the GABA B receptor is very important to clarify structural requirements. In that sense, we report the synthesis, binding studies and X-ray determinations of various 3- heteroaromatic γ-aminobutyric acids. Biochemical investigations concerning their abilities ...