Synthesis and anticonvulsant activity of two N-(2,6-dimethylphenyl)pyridinedicarboximides

Two N-(2,6-dimethylphenyl)pyridinedicarboximides were synthesized and evaluated for anticonvulsant properties and neurotoxicity. These compounds were mainly active against maximal electroshock (MES) induced seizures in animal models. In rats dosed orally, N-(2,6-dimethylphenyl-2,3-pyridinedicarboxim...

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Bibliographic Details
Published in:Biomedicine & pharmacotherapy 1995, Vol.49 (2), p.75-78
Main Authors: Bailleux, V, Vallée, L, Nuyts, J.P., Vamecq, J
Format: Article
Language:English
Subjects:
Animals
anticonvulsant activity
Anticonvulsants - chemical synthesis
Anticonvulsants - pharmacology
Anticonvulsants. Antiepileptics. Antiparkinson agents
Biological and medical sciences
Male
Medical sciences
Mice
Mice, Inbred Strains
N-(2,6-dimethylphenyl)pyridinedicarboximides
Neuropharmacology
neurotoxicity
Neurotoxins - chemical synthesis
Neurotoxins - pharmacology
Pharmacology. Drug treatments
Pyridines - chemical synthesis
Pyridines - pharmacology
Rats
Rats, Sprague-Dawley
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Summary:Two N-(2,6-dimethylphenyl)pyridinedicarboximides were synthesized and evaluated for anticonvulsant properties and neurotoxicity. These compounds were mainly active against maximal electroshock (MES) induced seizures in animal models. In rats dosed orally, N-(2,6-dimethylphenyl-2,3-pyridinedicarboximide 1 exhibited an anti-MES ED 50 of 54.2 μmol/kg and a protective index (PI = TD 50/ED 50) superior to 27.4. In mice dosed intraperitoneally, compound 1 is less active against MES induced seisure (ED 50 = 160.9 μmol/kg) and more neurotoxic as evidenced by a low protective index (1.93). Comparison with published data on phenytoin reveals that compound 1 is, in rats dosed orally, two-fold more potent than this antiepileptic drug against MES induced seizures.
ISSN:0753-3322
1950-6007
DOI:10.1016/0753-3322(96)82590-X