Synthesis and Evaluation of Anticonvulsant Activities of Triazole- Incorporated Benzothiazoles
Ming-Xia Song, Hong Zeng, Xian-Qing Deng and Zhe-Shan Quan
Pages 488-494 (7)
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.
Anticonvulsant, Benzothiazole, MES, Neurotoxicity, Rotorod, Triazole.
Medical College, Jinggangshan University, Ji'an, Jiangxi, 343009, China.