Document Report Card

ID: ALA1121465

Journal: J Med Chem

Title: New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide.

Authors: Kaplan JP, Raizon BM, Desarmenien M, Feltz P, Headley PM, Worms P, Lloyd KG, Bartholini G.

Abstract: Schiff bases of gamma-aminobutyric acid (gammaAbu) and gamma-aminobutyramide (gammaAbuNH2) were prepared and tested for anticonvulsant and gammaAbu mimetic activity. 4-[[(4-Chlorophenyl)(5-fluoro-2-hydroxyphenyl)methylene]amino]butanoic acid monosodium salt (4) and 4-[[(4-chlorophenyl)(5-fluoro-2-hydroxyphenyl)methylene]amino]butanamide (5) blocked bicuculline-induced lethality and convulsions and displaced [3H]gammaAbu from its membrane binding sites. In the rat dorsal root sensory ganglion, compound 4 exhibited gammaAbu agonist properties. Compounds 4 and 5 are thus anticonvulsants and directly acting gammaAbu mimetics.

CiteXplore: 7392039

DOI: 10.1021/jm00180a029