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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Evaluation of Anticonvulsant Activities of Triazole- Incorporated Benzothiazoles

Author(s): Ming-Xia Song, Hong Zeng, Xian-Qing Deng and Zhe-Shan Quan

Volume 11 , Issue 4 , 2014

Page: [488 - 494] Pages: 7

DOI: 10.2174/15701808113106660093

Price: $65

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.

Graphical Abstract

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