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Syntheses and GABA receptor binding properties of 4-amino-1-, 2-, and 3-hydroxybutylphosphinic acids

✍ Scribed by Jan Kehler; Bjarke Ebert; Otto Dahl; Povl Krogsgaard-Larsen

Publisher: Elsevier Science
Year: 1999
Tongue: French
Weight: 664 KB
Volume: 55
Category: Article
ISSN: 0040-4020
DOI: 10.1016/s0040-4020(98)01069-2

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✦ Synopsis

Novel racemic 4-amino-l-, 2-, and 3-hydroxybutylphosphinic acids and the corresponding 4-amino-1-, 2-, and 3-hydroxybutyl methylphosphinic acids have been synthesized. The phosphinic acid groups are bioisosteres of the carboxylic acid group, and some of these hydroxy amino acids are GABAB antagonists. The novel phosphinic acids were evaluated for their GABA^ and GABAB receptor binding properties using rat brain synaptosomes and were also tested for GABAergic activity in a guinea pig ileum model. None of the phosphinic acids tested were found to be active.

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