Abstract
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
Letters in Drug Design & Discovery
Title:Synthesis and Anticonvulsant Activity Evaluation of Some 1-alkoxy-4-(1H- 1,2,4-triazol-1-yl)phthalazines
Volume: 9 Issue: 4
Author(s): Shi-Ben Wang, Xian-Qing Deng, Ming-Xia Song, Zhe-Shan Quan
Affiliation:
Keywords: Anticonvulsant, 2, 3-Dihydrophthalazine-1, 4-dione, 1H-1, 2, 4-Triazole, Phthalazine, Maximal Electroshock, Neurotoxicity
Abstract: 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.
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Shi-Ben Wang, Xian-Qing Deng, Ming-Xia Song, Zhe-Shan Quan , Synthesis and Anticonvulsant Activity Evaluation of Some 1-alkoxy-4-(1H- 1,2,4-triazol-1-yl)phthalazines, Letters in Drug Design & Discovery 2012; 9 (4) . https://dx.doi.org/10.2174/157018012799860024
DOI https://dx.doi.org/10.2174/157018012799860024 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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