化学通报（印刷版）
化學通報（印刷版）
화학통보（인쇄판）
CHEMISTRY
2010年
2期
188-192
,共5页
抗癫痫活性%苯并氮杂(卓)%最大电惊厥
抗癲癇活性%苯併氮雜(卓)%最大電驚厥
항전간활성%분병담잡(탁)%최대전량궐
Anticonvulsant activities%Benzoazepin%Maximal Electroshock Seizure(MES)
合成了一系列1,3,4,5-四氢-7-烷氧基-2H-1-苯并氮杂(卓)-2-酮衍生物.采用最大电惊厥实验测定化合物的抗惊厥活性,其中的1,3,4,5-四氢-7-丁氧基-2H-1-苯并氮杂(卓)-2-酮(4b)具有较强的抗惊厥活性,ED_(50)为52.8 mg/kg,TD_(50)为246.2mg/kg,PI为4.7.
閤成瞭一繫列1,3,4,5-四氫-7-烷氧基-2H-1-苯併氮雜(卓)-2-酮衍生物.採用最大電驚厥實驗測定化閤物的抗驚厥活性,其中的1,3,4,5-四氫-7-丁氧基-2H-1-苯併氮雜(卓)-2-酮(4b)具有較彊的抗驚厥活性,ED_(50)為52.8 mg/kg,TD_(50)為246.2mg/kg,PI為4.7.
합성료일계렬1,3,4,5-사경-7-완양기-2H-1-분병담잡(탁)-2-동연생물.채용최대전량궐실험측정화합물적항량궐활성,기중적1,3,4,5-사경-7-정양기-2H-1-분병담잡(탁)-2-동(4b)구유교강적항량궐활성,ED_(50)위52.8 mg/kg,TD_(50)위246.2mg/kg,PI위4.7.
A series of 1,3,4,5-tetrahydro-7-alkoxy-2H-1-benzazepin-2-one derivatives were synthesized and characterized by ~1H NMR.MS and IR.Their anticonvulsant activities were screened by the maximal electroshock (MES)test.Among them 1,3,4,5-tetrahydro-7-butoxy-2H-1-benzazepin-2-one(4b)was found to be better anticonvulsant activity,ED_(50),TD_(50) and PI were 52.8 mg/kg,246.2mg/kg and 4.7,respectively.
