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.
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis; D002492:Central Nervous System Depressants / Q000138:chemical synthesis*; D005260:Female; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis; D010080:Oxazoles / Q000138:chemical synthesis*; D010424:Pentobarbital / Q000494:pharmacology; D051381:Rats; D012890:Sleep / Q000187:drug effects; D013997:Time Factors
D000927:Anticonvulsants; D002492:Central Nervous System Depressants; D007555:Isoxazoles; D008996:Monoamine Oxidase Inhibitors; D010080:Oxazoles; D010424:Pentobarbital