Synthesis Of 5-phenyl-3-pyrazolidinoses Derivants And Research Of Antiepileptic Activity

Now 70-80 percent seizure can be controlled by the rational and scientific use of antiepileptics (AEDs). However 20-25 percent seizure still remain being unable to control its attack. Some of them become the intractable epilepsy,which bring them heavy hearts and financial burden.The teachers and researchers in medicinal chemistry have been syntheticing 3-pyrazolidinones and doing research about antiepileptics for many years. They screened chemical compound with better activity and published some of them which laid a foundation for later research and development.In order to find antiepileptic with more effective affect and less toxic action and side effect,based on predecessors' research,3-pyrazolidinones was used as a lead compound in this study,and 13 new compounds of 3 kinds were designed and synthesized. The constitutional formulas are the following:Its structures were confirmed by IR,1H-NMR,MS and Elementary analysis. Its antiepileptic activity was measured with the convulsive method of maximal electricity. And the compounds was measured by usingPhenobarbital and Sodium Valproate as controls.The tests showed that 13 different of 3 kinds 3-pyrazo-lidinones had counteraction to MES to a different degree. The compounds 01-05 were prepared by leading Valproatyl derivants of Sodium valproate with antiepileptic activity into the first position of 5-substitutedphemyl -3-pyrazolidi-nones. Pharmacological tests showed:The derivant prepared by leading 4-methoxyl into the fifth position of benzol had better antiepileptic activity.The compounds 06-10 were prepared by leading cinna moyl derivants of N-cinnamoylpiperazine with antiepileptic activity into the first position of 5-substitu tedphemyl-3-pyazolidinones. Pharmacological tests showed:There were no significant difference on antiepileptic activity between the five new compounds and the five lead compounds.The compounds 11-13 were prepared by leading cinnamoyl derivants with antiepileptic activity into the second position of 5-phenyl-l-n-propyl-3-pyrazolidinones. The pharmacological activity of the new compounds were better than that of the lead compounds and best among the three kinds compound that we studied.