Synthesis of 3‐amino‐3,4‐dihydro‐2(1H)‐quinazolinones as potential anticonvulsants

Thirteen 3‐amino‐3,4‐dihydro‐2(1H)‐quinazolinones have been synthesized from ethyl chloroformate and o‐aminobenzylhydrazines. The latter compounds were obtained from the metal hydride reduction of either o‐aminobenzhydrazides or o‐acylaniline hydrazones. All compounds were evaluated in mice in the maximal electroshock (MES) seizure and pentylenetetrazole (sc Met) seizure threshold tests for anticonvulsant activity and in the rotorod test to determine neurotoxicity. Five of the compounds showed activity in one or both tests at a dose of 300 mg/kg or lower. The most active compound is 3‐dimethylamino‐3,4‐dihydro‐2(1H)‐quinazolinone.