Journal
MEDICINAL CHEMISTRY
Volume 6, Issue 5, Pages 313-320Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/157340610793358855
Keywords
Synthesis; triazole; benzo[d]thiazoles; anticonvulsant; maximal electroshock
Categories
Funding
- National Natural Science Foundation of China [30860340]
Ask authors/readers for more resources
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 (ED50) 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).
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available