Shineva N. Synthesis, phycal-chemical and pharmacological characteristics of N,N'-bisubstituted 2,3-dioxo-1,4-diazines.

A synthesis is carried out and potent anticonvulsants are got among the derivates of N,N'-disubstituted of 1,4-dihydropyrazine-2,3-diones. The method of synthesis of derivates of 1-aryl-1,4-dihydropyrazine-2,3-dions is developed by the intramolecular cyclization of 2,2-dimethoxyethylamides of oxanylic acids. Alkylation of 1-aryl-1,4-dihydropyrazine-2,3-dions with benzylchlorides is carried out in dimethylformamide. 1,4-disubstituted 2,3-dioxo-1,4-dihydropyrazines are synthesized by interaction of 1-substituted dihydropyrazine-2,3-dions with aryl(arylalkyl)chloracetic acid. Anticonvulsant activity of the substances synthesized was prognosed by the PASS-program. It is discovered as a result of pharmacological screening, that 3,4-dimethoxyphenylamide-4-[(3',4'-dimethoxyphenyl)-2,3-dioxo-1,4-dihydropyrazine-1-yl]acetic acid shows a high anticonvulsant activity which exceeds such Depakine. This substance is offered for preclinical research and for it the project of AND is developed.