New CNS-active 3-methyl-4-substituted methyl-delta 2-isoxazolin-5-ones

Eight 3-methyl-4-substituted methyl-delta 2-isoxazolin-5-ones were synthesized and evaluated for central nervous system (CNS) activity. All compounds at a concentration of 1 . 10(-3) mol/l inhibited rat brain monoamine oxidase (MAO) in vitro and provided protection against pentetrazole-induced convulsions in mice at a dose of 100 mg/kg i.p. Compounds 2 and 6 showed 80% protection. All isoxazolines (100 mg/kg i.p.) potentiated pentobarbital sleeping time in mice.