Literature DB >> 7392039

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

J P Kaplan, B M Raizon, M Desarmenien, P Feltz, P M Headley, P Worms, K G Lloyd, G Bartholini.   

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.

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Year:  1980        PMID： 7392039     DOI： 10.1021/jm00180a029

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  12 in total

1.  The 2011 E. B. Hershberg award for important discoveries in medicinally active substances: (1S,3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115), a GABA aminotransferase inactivator and new treatment for drug addiction and infantile spasms.

Authors:  Richard B Silverman
Journal:  J Med Chem       Date:  2012-01-10       Impact factor: 7.446

2.  Submassive hepatic necrosis associated with the use of progabide: a GABA receptor agonist.

Authors:  S J Munoz; R Fariello; W C Maddrey
Journal:  Dig Dis Sci       Date:  1988-03       Impact factor: 3.199

3.  A reversed-phase high-performance liquid chromatography assay procedure for progabide and its related metabolic derivatives.

Authors:  N F Farraj; S S Davis; G D Parr; H N Stevens
Journal:  Pharm Res       Date:  1987-02       Impact factor: 4.200

4.  The stability and solubility of progabide and its related metabolic derivatives.

Authors:  N F Farraj; S S Davis; G D Parr; H N Stevens
Journal:  Pharm Res       Date:  1988-04       Impact factor: 4.200

5.  Biphasic effects of direct, but not indirect, GABA mimetics and antagonists on haloperidol-induced catalepsy.

Authors:  P Worms; K G Lloyd
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1980-03       Impact factor: 3.000

6.  Isothiouronium compounds as gamma-aminobutyric acid agonists.

Authors:  R D Allan; H W Dickenson; B P Hiern; G A Johnston; R Kazlauskas
Journal:  Br J Pharmacol       Date:  1986-06       Impact factor: 8.739

7.  SL 75 102 as a gama-aminobutyric acid agonist: experiments on dorsal root ganglion neurones in vitro.

Authors:  M Desarmenien; P Feltz; P M Headley; F Santangelo
Journal:  Br J Pharmacol       Date:  1981-02       Impact factor: 8.739

8.  Phosphorus GABA Analogues as Potential Prodrugs.

Authors:  L A Cates; M S Rashed
Journal:  Pharm Res       Date:  1984-11       Impact factor: 4.200

9.  A facile synthesis of highly functionalized 4-arylcoumarins via Kostanecki reactions mediated by DBU.

Authors:  In-Taek Hwang; Sun-Ah Lee; Jin-Soo Hwang; Kee-In Lee
Journal:  Molecules       Date:  2011-07-26       Impact factor: 4.411

10.  Synthesis of new Schiff bases bearing 1,2,4-triazole, thiazolidine and chloroazetidine moieties and their pharmacological evaluation.

Authors:  Nadia G Kandile; Mansoura I Mohamed; Hind M Ismaeel
Journal:  J Enzyme Inhib Med Chem       Date:  2016-10-21       Impact factor: 5.051
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