Synthesis and Anticonvulsant Activity of 6‐Alkoxy‐[1,2,4]Triazolo[3,4‐a]Phthalazines |
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Authors: | Lei Zhang Li‐Ping Guan Xian‐Yu Sun Cheng‐Xi Wei Kyu‐Yun Chai Zhe‐Shan Quan |
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Affiliation: | 1. Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, Jilin Province, China;2. Department of Chemistry, Wonkwang University, Iksan 570‐749, Korea |
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Abstract: | A new series of 6‐alkoxy‐[1,2,4]triazolo[3,4‐a]phthalazines ( 3a – 3v ) were synthesized and their anticonvulsant activity and neurotoxicity were evaluated by the maximal electroshock test and the rotarod test respectively. Significant anticonvulsant activity was displayed by a number of compounds. The most promising compounds 6‐(4‐chlorobenzyloxy)‐[1,2,4]triazolo[3,4‐a]phthalazine ( 3f) and 6‐heptyloxy‐[1,2,4]triazolo[3,4‐a]phthalazine ( 3s) showed a median effective dose of 7.1 and 11.0 mg/kg, and had protective index value of 5.2 and 8.0 respectively. The two compounds were further found to have potent activity against seizures induced by pentylenetetrazole, isoniazid, thiosemicarbazide, 3‐mercaptopropionic acid but not seizures induced by strychnine, indicating that the two compounds might function by enhancing gamma‐aminobutyric acid neurotransmission. |
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Keywords: | anticonvulsant activity synthesis [1,2,4]triazolo[3,4‐a]‐phthalazines |
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