Journal of Medicinal Chemistry p. 702 - 704 (1980)
Update date:2022-09-26
Topics:
Kaplan
Raizon
Desarmenien
Feltz
Headley
Worms
Lloyd
Bartholini
Schiff bases of γ-aminobutyric acid (γAbu) and γ-aminobutyramide (γAbuNH2) were prepared and tested for anticonvulsant and γAbu 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]γAbu from its membrane binding sites. In the rat dorsal root sensory ganglion, compound 4 exhibited γAbu agonist properties. Compounds 4 and 5 are thus anticonvulsants and directly acting γAbu mimetics.
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