Synthesis Of Phthalide And Heterocyclic Compounds And The Antiepileptic Activity Study

Epilepsy is an unpleasant central nervous system disease, clinical using drug treatment for the first choice to treatment of epilepsy. However, the clinical existing antiepileptic drugs can not be well positioned to meet the needs of patients, research new antiepileptic drugs is of great significanceAim:Combined heterocyclic compounds with the phthalazine compounds, in order to obtain a high anti-epileptic activity, low neurotoxicity new compounds, to lay the foundation for new skeleton has independent intellectual property rights for the development of anti-epileptic drugs.Methods:Thirty-four compounds were synthesized using2,3-dihydrophthalazine-1,4-dione as the starting materials with reaction by chlorine reaction, hydrazinolysis reaction and other reactions. The synthesized compounds confirmed the structure using1H-NMR, IR and so on; Evaluation of the antiepileptic activity of the compound synthesized using the maximal electroshock seizures experiment, Evaluation of the neurotoxicity using the rotation method, Activity of the best compounds for a variety of chemical induced epilepsy model test.Results and Discussion:The phthalazine combined with heterocyclic compounds in the study, found that a compound of14having a high anti-epileptic activity, low neurotoxicity, its median effective dose against maximal electroshock seizures experiment is9.3mg/kg, at the same time, the compound demonstrates a lower neurotoxicity. Comprehensive evaluation of the compound is significantly superior to carbamazepine role.Conclusion:(1) Through to the split of the parent nucleus, make the antiepileptic activity increased;(2) Compound14would be the most effective compound of the this series compounds.(3) The research has certain reference significance and lay the foundation for further study.