AI Article Synopsis
- A new series of 7-substituted [1,2,4]triazolo[4,3-f]pyrimidine derivatives were created to explore their potential as anticonvulsant drugs.
- The compound 3i was identified as the most effective in the study with a median effective dose of 34.7 mg/kg and a protective index of 7.6, indicating it has a favorable safety profile.
- Additionally, compound 3i successfully reduced seizures caused by various triggers while demonstrating low oral neurotoxicity.
Article Abstract
In this study, a novel series of 7-substituted-[1,2,4]triazolo[4,3-f]pyrimidine derivatives was synthesized as potential anticonvulsant agents. Their anticonvulsant activities were evaluated by the maximal electroshock (MES) test, and their neurotoxicities were evaluated by the rotarod neurotoxicity test. The pharmacological results showed that the compound 3i (7-(4-chlorophenoxy)-[1,2,4]triazolo[4,3-f]pyrimidine) was among the most active agent with median effective dose (ED(50)) value of 34.7 mg/kg, median toxicity dose (TD(50)) of 262.9 mg/kg, and providing a protective index (PI=TD(50)/ED(50)) value of 7.6. The compound 3i also showed oral activity against MES-induced seizures and lower oral neurotoxicity. The compound 3i demonstrated antagonistic activity against seizures induced by PTZ, ISN, 3-MP and thiosemicarbazide.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.2174/1573406411208061076 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!