| Synthesis and Anticonvulsant Activities of Some Triazolothiadiazole Derivatives. | |
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MedLine Citation:
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PMID: 22532235 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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The present study describes the synthesis and anticonvulsant activity evaluation of 6-substituted-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives (4a-4x) and their partially dehydrogenated products 5,6-dihydro-6-substituted-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives (5a-5n). The bioevaluation demonstrated that most compounds in the series of 4a-4x exhibited potent anticonvulsant activity in the maximal electroshock test. Among which, 6-(4-chlorophenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (4h) emerged as the most promising candidate on the basis of its favorable ED(50) value of 23.7 mg/kg and PI value of 10.8. In addition, the potency of compound 4h against seizures induced by pentylenetetrazole, 3-mercaptopropionic acid, and bicuculline in the chemical-induced seizure tests suggested that compound 4h displayed broad-spectrum activity in several models, and it may exert its anticonvulsant activity through affecting the GABAergic system. |
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Authors:
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Xian-Qing Deng; Zheng-Qi Dong; Ming-Xia Song; Bing Shu; Shi-Ben Wang; Zhe-Shan Quan |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-4-25 |
Journal Detail:
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Title: Archiv der Pharmazie Volume: - ISSN: 1521-4184 ISO Abbreviation: - Publication Date: 2012 Apr |
Date Detail:
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Created Date: 2012-4-25 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0330167 Medline TA: Arch Pharm (Weinheim) Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. |
Affiliation:
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College of Pharmacy, Yanbian University, Yanji, Jilin, China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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