Abstract

The thiosemicarbazone of acetophenone ( 1a) had been shown previously to afford protection against experimentally-induced seizures. This report describes the systematic chemical modification of 1a and the activities of these analogues in the maximal electroshock seizure (MES) test, subcutaneous maximal pentylenetetrazole seizure (scPTZ) test and neurotoxicity screen in mice when administered by the intraperitoneal route. Most of the compounds were active and representative compounds examined for oral activity in rats revealed that in most cases protection against seizures induced in the MES screen but not the scPTZ test was achieved at a dose of 50 mg/kg. Some correlations between chemical structures and anticonvulsant properties were found.

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