Anticonvulsant activity of some 4-aminophenylacetamides.

doi:10.1002/JPS.2600760106

Paper

Anticonvulsant activity of some 4-aminophenylacetamides.

Published 1987 · C. R. Clark, T. Davenport

Journal of pharmaceutical sciences

Q2 SJR score

10

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Abstract

A series of 4-aminophenylacetamides was prepared and evaluated for anticonvulsant activity. These compounds were prepared during studies designed to determine the relationship between benzamide-like compounds and anticonvulsant effects. Unlike benzamides, these phenylacetamides have a methylene group between the aromatic ring and the amide carbonyl. Consequently, formal conjugation is lost, and the number of conformational degrees of freedom has increased. The compounds were tested in mice against seizures induced by electroshock and pentylenetetrazol, and in the rotorod assay for neurologic deficit. The more active and selective anticonvulsants prepared in this study were those having an additional aromatic ring as part of the substituent on the amide nitrogen. Compound 16, the 4-aminophenylacetamide derived from 2,6-dimethylaniline, was the most potent compound observed (ED50 = 50.50 mg/kg against electroshock-induced convulsions and ED50 = 93.20 mg/kg against pentylenetetrazol-induced convulsions).

Non-RCT

Animal Study

Study Snapshot

4-aminophenylacetamides with additional aromatic rings as part of the substituent on the amide nitrogen show more active and selective anticonvulsant properties, with compound 16 being the most potent.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Paper

Anticonvulsant activity of some 4-aminophenylacetamides.

References

Anticonvulsant activity of 2- and 3-aminobenzanilides.

3-aminobenzanilide 21, derived from 2,6-dimethylaniline, shows the most potent anticonvulsant activity, comparable to phenobarbital and phenytoin.

Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy.

6-aryl-3-(hydroxypolymethyleneamino)pyridazines derivatives show potential anticonvulsant activity, with compounds like 6-(2-chlorophenyl)-3-(4-hydroxypiperidino)pyridazine (2) and 6-(2,4-d

Anticonvulsant activity of some 4-aminobenzamides.

4-aminobenzamides show promising anticonvulsant activity, with d,l-4-amino-N-(alpha-methylbenzyl)-benzamide (12) showing the highest activity compared to phenobarbital and phenytoin in mouse models.

Synthesis and anticonvulsant activity of some substituted lactams and amides.

Substituted lactams and amides, such as 3-hydroxy-1-methyl-3-phenyl-2-piperidinone and 3-methoxy-3-phenyl-2-piperidinone, show anticonvulsant activity comparable to valproic acid.

Multiple Dopamine Receptors in Brain and the Pharmacological Action of Substituted Benzamide Drugs

Substituted benzamide drugs selectively block brain dopamine receptors, with their receptor interaction depending on the presence of sodium ions, potentially improving schizophrenia treatment.

Citations