Synthesis and anticonvulsant evaluation of some novel 4(3H)-quinazolinones

A series of novel quinazoline derivatives, methaqualone analogs, were synthesized, evaluated for their anticonvulsant activity against electrically and chemically (pentylenetetrazole, picrotoxin, and strychnine) induced seizures and compared with the standard drugs methaqualone and sodium valproate. 3,4-Dihydro-2-methyl-3-(2-methylphenyl)-4-oxoquinazolin-8-yl propanoate, benzenesulfonate, and 4-nitrobenzenesulfonate as well as 2-methyl-3-(2-methylphenyl)-8-methoxy-4(3H)-quinazolinone and 2-[3,4-dihydro-2-methyl-3-(2-methylphenyl)-4-oxoquinazolin-8-yloxy]acetic acid hydrazide were found to be the most potent compounds of this series accompanied with relatively low neurotoxicity and low toxicity in the median lethal dose test as compared with the reference drugs.