Synthesis and Anticonvulsant Activity Evaluation of Some 1-alkoxy-4-(1H- 1,2,4-triazol-1-yl)phthalazines

Author(s): Shi-Ben Wang, Xian-Qing Deng, Ming-Xia Song, Zhe-Shan Quan

Journal Name: Letters in Drug Design & Discovery

Volume 9 , Issue 4 , 2012

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A series of 1-alkoxy-4-(1H-1,2,4-triazol-1-yl)phthalazine derivatives were synthesized using 2,3- dihydrophthalazine-1,4-dione as starting material. The structures of the compounds were characterized by elemental analysis, IR, 1H-NMR and MS data. Anticonvulsant activities of these compounds were evaluated by maximal electroshock (MES) test following intraperitoneal injection in mice. Among the synthesized compounds 3a-3t, compound 3e was the most active compound with an ED50 of 28.9 mg/kg, TD50 of 173.6 mg/kg and protective index (PI) of 6.0.

Keywords: Anticonvulsant, 2, 3-Dihydrophthalazine-1, 4-dione, 1H-1, 2, 4-Triazole, Phthalazine, Maximal Electroshock, Neurotoxicity

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Article Details

Year: 2012
Published on: 26 April, 2012
Page: [409 - 414]
Pages: 6
DOI: 10.2174/157018012799860024
Price: $65

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