EVALUATION OF THE THIOSEMICARBAZONES OF SOME ARYL ALKYL KETONES AND RELATED-COMPOUNDS FOR ANTICONVULSANT ACTIVITIES

被引：40

作者：

DIMMOCK, JR ^{[1
]}

MCCOLL, JM ^{[1
]}

WONKO, SL ^{[1
]}

THAYER, RS ^{[1
]}

HANCOCK, DS ^{[1
]}

机构：

[1] UNIV SASKATCHEWAN,TOXICOL RES CTR,SASKATOON S7N 0W0,SASKATCHEWAN,CANADA

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 26卷 / 05期

关键词：

THIOSEMICARBAZONES OF KETONES; ANTICONVULSANT ACTIVITIES; STRUCTURE-ACTIVITY RELATIONSHIPS;

D O I：

10.1016/0223-5234(91)90148-G

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The thiosemicarbazone of acetophenone (1a) had been shown previously to afford protection against experimentally-induced seizures. This report describes the systematic chemical modification of 1a and the activities of these analogues in the maximal electroshock seizure (MES) test, subcutaneous maximal pentylenetetrazole seizure (scPTZ) test and neurotoxicity screen in mice when administered by the intraperitoneal route. Most of the compounds were active and representative compounds examined for oral activity in rats revealed that in most cases protection against seizures induced in the MES screen but not the scPTZ test was achieved at a dose of 50 mg/kg. Some correlations between chemical structures and anticonvulsant properties were found.

引用

页码：529 / 534

页数：6

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