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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
VOLUME: 11
ISSUE: 4
DOI: 10.2174/15701808113106660093      Price:  $58









Synthesis and Evaluation of Anticonvulsant Activities of Triazole- Incorporated Benzothiazoles

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Author(s): Ming-Xia Song, Hong Zeng, Xian-Qing Deng and Zhe-Shan Quan
Pages 488-494 (7)
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.
Affiliation:
Medical College, Jinggangshan University, Ji'an, Jiangxi, 343009, China.