Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis and Evaluation of Anticonvulsant Activities of Triazole- Incorporated Benzothiazoles

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

Graphical Abstract:


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.

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Article Details

VOLUME: 11
ISSUE: 4
Year: 2014
Page: [488 - 494]
Pages: 7
DOI: 10.2174/15701808113106660093
Price: $58