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具有抗惊厥活性的新型琥珀酸环衍生物的合成与性质

Synthesis and properties of new cyclic derivatives of succinic acid with anticonvulsant activity.

作者信息

Lange J, Rump S, Galecka E, Ilczuk I, Lechowska-Postek M, Rabsztyn T

出版信息

Pharmazie. 1977 Feb;32(2):82-4. doi: 10.1002/chin.197728159.

Abstract

The synthesis and pharmacological screening of a series of new phenylsuccinimide derivatives are described. Seven compounds of that series elicited a marked anticonvulsant activity. Among the compounds tested, interesting structures were those metasubstituted with bromine, fluorine or trifluoromethyl group. The most interesting drug seems to be the N-morpholinemethyl derivative of mbromophenylsuccinimide, which has a long duration of activity, elicits a very strong antipentetrazole action, and gives good protection against maximal electroshock seizures.

摘要

描述了一系列新型苯基琥珀酰亚胺衍生物的合成及药理筛选。该系列中的七种化合物表现出显著的抗惊厥活性。在测试的化合物中,有趣的结构是那些被溴、氟或三氟甲基间位取代的结构。最有趣的药物似乎是间溴苯基琥珀酰亚胺的N-吗啉甲基衍生物,它具有较长的活性持续时间,引发非常强的抗戊四氮作用,并对最大电休克惊厥提供良好的保护。

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