957950-80-0Relevant academic research and scientific papers
Synthesis of 2-Substituted-7-heptyloxy-4,5-dihydro-[1,2,4]-triazolo[4,3-a] quinolin-1(2H)-ones with Anticonvulsant Activity
Wei, Cheng-Xi,Li, Fu-Nan,Zhao, Long-Xuan,Zhao, Li-Ming,Quan, Zhe-Shan
, p. 491 - 495 (2007)
A series of 2-substituted-7-heptyloxy-4,5-dihydro-[1,2,4]triazolo[4,3-a] quinolin-1(2H)-ones was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test, subcutaneous pentylenetetrazol (sc-PTZ), and rotarod tests with intraperitoneally injected mice. Among the synthesized compounds, 2-propionyl-7-heptyloxy-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline-1(2H)-one 4b was the most active one and also had the lowest toxicity. In the anti-MES potency test, it showed median effective dose (ED50) of 8.2 mg/kg, median toxicity dose (TD50) of 318.3 mg/kg, and the protective index (PI) of 39.0 which is much greater than the PI of the reference drugs phenytoin and carbamazepine.
