Syntheses and Gaba Receptor Binding Properties of 1-, 2- and 3-Hydroxy Aminobutyl Phosphinic Acids

Abstract

Novel racemic 1-hydroxy-, 2-hydroxy- and 3-hydroxy aminobutyl-phosphinic and metylphosphinic acids were synthesized. The acids are bioisosteres of the corresponding carboxylic acids, some of which are GABA, antagonists. The novel hydroxylated phosphinic and methylphosphinic acids were evaluated for their GABA, and GABA, receptor binding properties using rat brain synaptosomes and were also tested for GABA activity in a guinea pig ileum model. All the compounds tested were inactive.