Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of gamma-aminobutyric acid acting as selective GABA-A antagonists.

@article{Wermuth1987SynthesisAS,
  title={Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of gamma-aminobutyric acid acting as selective GABA-A antagonists.},
  author={Camille G. Wermuth and Jean Jacques Bourguignon and Gilbert Schlewer and J P Gies and Ang{\`e}le Schoenfelder and A M Meliki{\`a}n and M J Bouchet and D Chantreux and Jerome Molimard and M. de Heaulme},
  journal={Journal of medicinal chemistry},
  year={1987},
  volume={30 2},
  pages={239-49}
}
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 compounds displaced [3H]GABA from rat brain membranes. All the active… CONTINUE READING