1,4-苯二氮䓬衍生物的合成及药理活性
Synthesis and pharmacological activity of 1,4-benzodiazepine derivatives.
作者信息
Osman A N, el-Gendy A A, Omar R H, Wagdy L, Omar A H
机构信息
Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
出版信息
Boll Chim Farm. 2002 Jan-Feb;141(1):8-14.
PMID:12064063
Abstract
2-Aminobenzamides (3a-g) were prepared starting with isatoic anhydride. These compounds reacted with chloroacetic acid to give (4a-g), which were cyclized by dicyclohexylcorbodiimide to afford (5a-g). The preliminary pharmacological screening revealed that some of the new 2H-1,4-benzodiazepin-3,5(1H,4H)-dione derivatives (5) exhibited CNS-depressant and anticonvulsant activities.
摘要
2-氨基苯甲酰胺（3a-g）以邻苯二甲酸酐为起始原料制备。这些化合物与氯乙酸反应得到（4a-g），（4a-g）再经二环己基碳二亚胺环化得到（5a-g）。初步药理筛选表明，一些新型2H-1,4-苯并二氮杂卓-3,5(1H,4H)-二酮衍生物（5）具有中枢神经系统抑制和抗惊厥活性。
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