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 : 14 | Download : 8

Publication Date : 0000-00-00

Article Type : Research Paper

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 insert ignore into journalissuearticles values(MES); test and 7-methoxy-5-phenyl-1,2,4-triazolo[4,3-a]quinoline insert ignore into journalissuearticles values(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 insert ignore into journalissuearticles values(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 insert ignore into journalissuearticles values(sc-PTZ); test, and isoniazid test. Compound 4a had a higher protective index insert ignore into journalissuearticles values(PI = TD50/ED50); value insert ignore into journalissuearticles values(16.6); than phenytoin insert ignore into journalissuearticles values(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