Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of. gamma.-aminobutyric acid acting as selective GABA-A antagonists
CG Wermuth, JJ Bourguignon, G Schlewer…
文献索引：Wermuth, Camille-Georges; Bourguignon, Jean-Jacques; Schlewer, Gilbert; Gies, Jean-Pierre; Schoenfelder, Angele; et al. Journal of Medicinal Chemistry, 1987 , vol. 30, # 2 p. 239 - 249
We have recently shown that an arylaminopyridazine derivative of GABA, SR 95103 [2-(3- carboxypropyl)-3-amino-4-methyl-6-phenylpyridazinium chloride], is a selective and competitive GABA-A receptor antagonist. In order to further explore the structural requirements for GABA receptor affinity, we synthesized a series of 38 compounds by attaching various pyridazinic structures to GABA or GABA-like side chains. Most of the ...
