2-和3-氨基苯甲酰苯胺的抗惊厥活性。

Anticonvulsant activity of 2- and 3-aminobenzanilides.

作者信息

Clark C R, Lin C M, Sansom R T

出版信息

J Med Chem. 1986 Aug;29(8):1534-7. doi: 10.1021/jm00158a038.

Abstract

A series of 2- and 3-aminobenzanilides derived from ring-alkylated anilines were prepared and evaluated for anticonvulsant activity. These benzanilides were prepared in the course of studies designed to determine the relationship between the benzamide structure and anticonvulsant effects. The compounds were tested in mice against seizures induced by maximal electroshock (MES) and pentylenetetrazole and in the rotorod assay for neurologic deficit. The 3-aminobenzanilide derived from 2,6-dimethylaniline, 21, was the most potent anti-MES compound, with an ED50 of 13.48 mg/kg and a protective index of 21.11 (PI = TD50/ED50). The activity profile for 21 compares favorably with that for phenobarbital and phenytoin.

摘要

制备了一系列由环烷基化苯胺衍生而来的2-氨基和3-氨基苯甲酰苯胺，并对其抗惊厥活性进行了评估。这些苯甲酰苯胺是在旨在确定苯甲酰胺结构与抗惊厥作用之间关系的研究过程中制备的。在小鼠中测试了这些化合物对最大电休克（MES）和戊四氮诱导的惊厥的作用，并在转棒试验中测试了其对神经功能缺损的影响。由2,6-二甲基苯胺衍生而来的3-氨基苯甲酰苯胺（21）是最有效的抗MES化合物，其半数有效剂量（ED50）为13.48 mg/kg，保护指数为21.11（PI = TD50/ED50）。21的活性谱与苯巴比妥和苯妥英的活性谱相比具有优势。