In:
Archiv der Pharmazie, Wiley, Vol. 348, No. 8 ( 2015-08), p. 564-574
Abstract:
A series of 4‐(substituted‐phenyl)‐[1,2,4]triazolo[4,3‐ a ]quinazolin‐5(4 H )‐ones ( 6a–x ) with triazole and other heterocyclic substituents ( 7–14 ) were synthesized and the compounds were evaluated for their anticonvulsant activity and neurotoxicity by maximal electroshock (MES) and rotarod neurotoxicity tests. Among the compounds studied, 6o and 6q showed wide margins of safety with protective indices (PIs) that were much higher than those of currently used drugs (PI 6o 〉 25.5, PI 6q 〉 26.0). Compounds 6o and 6q showed significant oral activity against MES‐induced seizures in mice, with ED 50 values of 88.02 and 94.6 mg/kg, respectively. The two compounds were also found to have potent activity against seizures that were induced by pentylenetetrazole and bicuculline.
Type of Medium:
Online Resource
ISSN:
0365-6233
,
1521-4184
DOI:
10.1002/ardp.201500115
Language:
English
Publisher:
Wiley
Publication Date:
2015
detail.hit.zdb_id:
1496815-0
SSG:
15,3