AI Article Synopsis
- A series of benzylamides derived from isocyclic and heterocyclic acids was synthesized and evaluated for their anticonvulsant properties in a study by the NIH.
- Almost all derivatives of heterocyclic acids displayed anticonvulsant activity, while isocyclic acid derivatives were found to be inactive.
- Notably, 2-furoic acid benzylamide demonstrated the most promise, showing effective results in seizure tests with a favorable protective index.
Article Abstract
A series of benzylamides of isocyclic and heterocyclic acids was synthesized and tested in Anticonvulsant Screening Project (ASP) of Antiepileptic Drug Development Program (ADDP) of NIH. Near all synthesized derivatives of heterocyclic acids showed activity. All obtained derivatives of mono- and bicyclic isocyclic acids were inactive. The power of action of heterocyclic acids derivatives seems does not depend upon kind of heteroatom (N, O or S). One of the compounds (2-furoic acid benzylamide (4)) appeared most promising. It showed in minimal clonic seizure (6Hz) test (ASP) in rats after i. p. administration: MES ED50 = 36.5 mg/kg, TOX TD50 = 269.75 mg/kg, and PI = 7.39.
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