Substituted (.omega.-aminoalkoxy)stilbene derivatives as a new class of anticonvulsants

A series of substituted (omega- aminoalkoxy )stilbene derivatives has been synthesized and screened for anticonvulsant activity. The effect of structural modification of these molecules on the activities has been systematically examined. Potent anticonvulsant activity was displayed by 2-[4-(4-methyl...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1984-05, Vol.27 (5), p.645-649
Main Authors: Kikumoto, Ryoji, Tobe, Akihiro, Fukami, Harukazu, Ninomiya, Kunihiro, Egawa, Mitsuo
Format: Article
Language:English
Subjects:
Animals
Anticonvulsants - chemical synthesis
Biological and medical sciences
Biological Assay
Drug Evaluation, Preclinical
Electroshock
General pharmacology
Indicators and Reagents
Male
Medical sciences
Mice
Mice, Inbred Strains
Pentylenetetrazole - toxicity
Pharmacology. Drug treatments
Physicochemical properties. Structure-activity relationships
Rats
Rats, Inbred Strains
Seizures - drug therapy
Stilbenes - chemical synthesis
Stilbenes - toxicity
Structure-Activity Relationship
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Summary:A series of substituted (omega- aminoalkoxy )stilbene derivatives has been synthesized and screened for anticonvulsant activity. The effect of structural modification of these molecules on the activities has been systematically examined. Potent anticonvulsant activity was displayed by 2-[4-(4-methyl-1 piperazinyl)butoxy]stilbene (20) and some 2-[4-(3-alkoxy-1-piperidino)butoxy]stilbene derivatives (21, 37, 38, and 40), as determined by maximal electroshock seizure (MES) and pentylenetetrazol-induced convulsion tests in mice. Compound 21 exhibited more potent anti-MES activity than diphenylhydantoin and carbamazepine in further pharmacological tests in rats, and its therapeutic index was superior to those of two antiepileptic drugs.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00371a015