1485056-65-2Relevant academic research and scientific papers
Synthesis and anticonvulsant evaluation of some new 1,3,4,5-tetrahydro-6- Alkoxy-2H-1-benzazepin-2-one derivatives
Han, Rong-Bi,Shao, Yun-Peng,Wu, Hui-Fan,Zhang, Duo,Piao, Feng-Yu
, p. 2810 - 2820 (2014/05/06)
A series of new 1,3,4,5-tetrahydro-6-Alkoxy-2H-1-benzazepin-2-one derivatives were synthesized and screened for their anticonvulsant activities by the maximal electroshock (MES) test, subcutaneous pentylenetetrazol (scPTZ) test, and their neurotoxicity was evaluated by the rotarod neurotoxicity test. The results of these tests showed that 1,3,4,5-tetrahydro-6-octyloxy-2H-1- benzazepin-2-one (4f) was the most promising compound, with median effective dose (ED50) of 20.4 mg/kg, and protective index (PI) value of 20.1 in the MES test, which is much higher than the PI value of the prototype antiepileptic drug carbamazepine (PI = 8.1), phenytoin (PI = 6.9), phenobarbital (PI = 3.2), and sodium valproate (PI = 1.6). The scPTZ test displayed that 1,3,4,5-tetrahydro-6-heptyloxy-2H-1-benzazepin-2-one (4e) was the most active compound (ED50 = 64.4, PI = 2.6). The possible structure-Activity relationship was discussed.
