- Turkish Journal of Chemistry
- Vol: 32 Issue: 2
- The Synthesis and Anticonvulsant Activity of 1-Substituted-7-Methoxy-1,2,4-Triazolo [4, 3-a]Quinolin...
The Synthesis and Anticonvulsant Activity of 1-Substituted-7-Methoxy-1,2,4-Triazolo [4, 3-a]Quinoline
Authors : Li-ping Guan, Xian-yu Sun, Guan-rong Tian
Pages : 181-189
View : 13 | Download : 7
Publication Date : 9999-12-31
Article Type : Makaleler
Abstract :A new series of 1-substituted-7-methoxy-5-phenyl-1,2,4-triazolo [4,3-a]quinolines were synthesized using ethyl-3-oxo-3-phenylpropanoate and 4-methoxybenzenamine as the starting material. Their anticonvulsant activity was evaluated by the maximal electroshock (MES) test and 7-methoxy-5-phenyl-1,2,4-triazolo[4,3-a]quinoline (4a) was identified as the most potent compound, with an ED50 value of 9.2 mg kg-1, which is comparable to the reference drug phenytoin (ED50 = 9.9 mg kg-1). To explore the possible mechanism of its anticonvulsant activity, compound 4a was tested with the rotarod neurotoxicity test, pentylenetetrazole (sc-PTZ) test, and isoniazid test. Compound 4a had a higher protective index (PI = TD50/ED50) value (16.6) than phenytoin (PI = 7.0), and it antagonized pentylenetetrazole- and isoniazid-induced seizures with an ED50 of 21.1 mg kg-1 and 83.3 mg kg-1, respectively.Keywords : 1, 2, 4-triazolo[4, 3-a] quinoline, Anticonvulsant, MES, sc-PTZ, Isoniazid