Synthesis and neuropharmacological activity of some quinoxalinone derivatives
Eight quinoxalinone derivatives were synthesized and investigated for some neuropharmacological effects (analgesia, sedation, convulsion, anxiety, memory and psychosis) in mice and rats. In the CNS depressant activity, N,N-dibenzyl-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonamide is the most active, while the other compounds appear variously dose-dependent. Only three of the compounds showed anxiolytic effect, with N,N-dibenzyl-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonamide showing the highest activity at 2.5 mg/kg. At the dose of 30 mg/kg, 6-nitro-1,4-dihydroquinoxaline-2,3-dione showed a better anxiolytic effect in mice than diazepam (dose: 1 mg/kg), while 1,2,3,4-tetrahydroquinoxaline-2,3-dione (dose: 25 mg/kg) showed a comparative effect to diazepam. 6-Chloro-1,4-dihydro-quinoxaline-2,3-dione and N,N-dibenzyl-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonamide showed significant anticonvulsant action. None of the compounds showed any analgesic or antidopaminergic effect. The LD50 (24 h) calculated for the compounds were between 74 and 160 mg/kg i.p.