Synthesis and anticonvulsant activity of 7-alkoxy-triazolo-[3, 4-b]benzo[d]thiazoles.

Xian-Qing Deng, Ming-Xia Song, Cheng-Xi Wei, Fu-Nan Li, Zhe-Shan Quan

College of Pharmacy, Yanbian University, No. 977 Park Road, Yanji, Jilin, China.

Medicinal chemistry (Shāriqah (United Arab Emirates)) 2010 Sep

filter terms:

The present study describes the chemical synthesis and anticonvulsant activity evaluation of a series of 7-alkoxy-triazolo-[3, 4-b]benzo[d]thiazoles. Most compounds exhibited good anticonvulsant activity in the Maximal electroshock (MES) test. And the structure-activity relationships (SAR) were analyzed. Among the compounds studied, 7-octyloxy-triazolo-[3, 4-b]benzo[d]thiazole (5g) was found to be the most potent compound with a median effective dose (ED(50)) value of 8.0 mg/kg and a protective index (PI) value of 15.0, possessing better anticonvulsant activity and higher safety than marketed drugs carbamazepine and phenytoin. The mechanism study of compound 5g showed that it displayed broad spectrum activity in several models, and it is likely to have several mechanisms of action (including inhibiting voltage-gated ion channels and GABAergic activity).

Citation

Xian-Qing Deng, Ming-Xia Song, Cheng-Xi Wei, Fu-Nan Li, Zhe-Shan Quan. Synthesis and anticonvulsant activity of 7-alkoxy-triazolo-[3, 4-b]benzo[d]thiazoles. Medicinal chemistry (Shāriqah (United Arab Emirates)). 2010 Sep;6(5):313-20