Abstract
A series of 6-alkoxy-2-(4H-1,2,4-triazol-4-yl)benzothiazoles was synthesized and evaluated for their anticonvulsant activity using the maximal electroshock (MES) method. Interestingly, all of the compounds prepared showed long duration of protection effect in the MES screens. And none of them, except compounds 4b and 4d, showed any neurotoxicity at dose of 300 mg/kg. Compound 4c was considered as the most promising one with an ED50 value of 39.4 mg/kg, and a superior PI value of 17.3 when compared to the marketed antiepileptic drugs carbamazepine, phenobarbital, and valproate. What’s more, compound 4c showed high protection against seizures induced by pentylenetetrazole.
Keywords: Anticonvulsant, Benzothiazole, MES, Neurotoxicity, Rotorod, Triazole.
Letters in Drug Design & Discovery
Title:Synthesis and Evaluation of Anticonvulsant Activities of Triazole- Incorporated Benzothiazoles
Volume: 11 Issue: 4
Author(s): Ming-Xia Song, Hong Zeng, Xian-Qing Deng and Zhe-Shan Quan
Affiliation:
Keywords: Anticonvulsant, Benzothiazole, MES, Neurotoxicity, Rotorod, Triazole.
Abstract: A series of 6-alkoxy-2-(4H-1,2,4-triazol-4-yl)benzothiazoles was synthesized and evaluated for their anticonvulsant activity using the maximal electroshock (MES) method. Interestingly, all of the compounds prepared showed long duration of protection effect in the MES screens. And none of them, except compounds 4b and 4d, showed any neurotoxicity at dose of 300 mg/kg. Compound 4c was considered as the most promising one with an ED50 value of 39.4 mg/kg, and a superior PI value of 17.3 when compared to the marketed antiepileptic drugs carbamazepine, phenobarbital, and valproate. What’s more, compound 4c showed high protection against seizures induced by pentylenetetrazole.
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Song Ming-Xia, Zeng Hong, Deng Xian-Qing and Quan Zhe-Shan, Synthesis and Evaluation of Anticonvulsant Activities of Triazole- Incorporated Benzothiazoles, Letters in Drug Design & Discovery 2014; 11 (4) . https://dx.doi.org/10.2174/15701808113106660093
DOI https://dx.doi.org/10.2174/15701808113106660093 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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