Synthesis and neuropharmacological activity of some quinoxalinone derivatives
Year: 2007
Type: article
Abstract: 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-2,3dione 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-1,4dihydro-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 LD 50 (24 h) calculated for the compounds were between 74 and 160 mg/kg i.p.
Source: HAL
Authors: Gbola Olayiwola, C.A. Obafemi, F. O. Taiwo
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
OpenAlex ID: W2161532279