Synthesis and anticonvulsant activity evaluation of 6-substituted-[1,2,4]triazolo[3,4-a](tetrazolo[5,1-a]) phthalazine derivatives

作者：Bian, Ming; Deng, Xian-Qing; Gong, Guo-Hua; Wei, Cheng-Xi; Quan, Zhe-Shan^*

来源：Journal of Enzyme Inhibition and Medicinal Chemistry, 2013, 28(4): 792-800.

DOI：10.3109/14756366.2012.684052

• Triazole
• Tetrazole
• Phthalazine
• Anticonvulsant
• Maximal electroshock

With the aim of finding new anticonvulsant drugs, new 6-substituted-[1,2,4] triazolo[3,4-a] (tetrazolo[5,1-a]) phthalazine derivatives (1-34) have been designed and synthesized. All the compounds were evaluated for their anticonvulsant activities using the maximal electroshock test (MES). Most of the synthesized compounds exhibited potent anticonvulsant activities in the MES. The most promising compound 14 showed significant anticonvulsant activity in MES test with ED50 value of 9.3 mg/kg. It displayed a wide margin of safety with protective index much higher than the standard drug Carbamazepine. And the potency of compound 14 against seizures induced by Pentylenetetrazole, Isoniazid, Thiosemicarbazide and 3-Mercaptopropionic acid in the chemical-induced seizure tests suggested that compound 14 displayed wide spectrum of activity in several models.

• 单位
  延边大学; 内蒙古民族大学