The Synthesis Of 9-benzy1-5,7-dimethy1-5H-tetrazolo[1,5-e]Purine-6,8(7H, 9H)-dione And Anticonvulsant Activity Study

A series of 9-benzyl-5,7-dimethyl-5H-tetrazolo[1,5-e]purine-6,8(7H,9H)-dione (4a-4s) were designed and synthesized. In order to appraise the effect of the anticonvulsant and neurotoxicity of the compounds, we used the method that MES, which is called the Maximal Electroshock test in the world, and gave compounds to the mice with intraperitoneal injection making them walking in the spinning wood with regularly speed. The conclusion and the results of pharmacology told us that most of the compounds we have synthesized showed so-so positive anticonvulsive activity. Among the compounds we’ve synthesized,the 9-benzyl-5,7-dimethyl-5H-tetrazolo[1,5-e]purine-6,8(7H,9H)-dione (41) has the greatest potent,because of the data of its ED50 value of 22.38 mg/kg and protect index (PI= TD50/ED50) value of 10.23. Not only the efficacy of the anti-MES, but also the potency of compound 41 opposing the seizures causing by pentylenetetrazole was also founded by us, Maybe, however, as suggested that the mechanisms of action including enhancing of GABAergic activity was involved in its anticonvulsant activity.