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对氯苯基取代的芳基氨基脲的抗惊厥活性——伯端氨基的作用

Anticonvulsant activity of p-chlorophenyl substituted arylsemicarbazones--the role of primary terminal amino group.

作者信息

Pandeya S N, Mishra V, Ponnilavarasan I, Stables J P

机构信息

Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, India.

出版信息

Pol J Pharmacol. 2000 Jul-Aug;52(4):283-90.

Abstract

A series of p-chlorophenyl substituted arylsemicarbazones were synthesized and evaluated for anticonvulsant activity. Most of the compounds provided significant protection against maximal electroshock-induced seizures (MES) at 100 mg/kg after 0.5 h and at 300 mg/kg after 4 h in both MES and pentetrazole-induced (PTZ) seizures. In the strychnine-induced seizures (scSTY), the majority of the compounds showed protection at 30 mg/kg. The compound 2 was active in both MES and PTZ tests. The study has shown that the terminal primary amino group is not necessary for anticonvulsant activity.

摘要

合成了一系列对氯苯基取代的芳基氨基脲,并对其抗惊厥活性进行了评估。在最大电休克诱导惊厥(MES)模型中,大多数化合物在给药0.5小时后100mg/kg剂量以及4小时后300mg/kg剂量时均能提供显著保护;在戊四氮诱导惊厥(PTZ)模型中,同样在上述剂量下也能提供显著保护。在士的宁诱导惊厥(scSTY)模型中,大多数化合物在30mg/kg剂量时表现出保护作用。化合物2在MES和PTZ试验中均有活性。研究表明,末端伯氨基对于抗惊厥活性并非必需。

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