Synthesis and anticonvulsant activity of some new hexahydropyrimidine-2,4-dione derivatives

被引:0
|
作者
Septioglu, E [1 ]
Aytemir, MD [1 ]
Çalis, Ü [1 ]
机构
[1] Hacettepe Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06100 Ankara, Turkey
来源
ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH | 2005年 / 55卷 / 05期
关键词
antiepileptic drugs; 6-arylhexahydropyrimidine 2,4-diones, anticonvulsant activity; S-alkylation; synthesis; carbamodithioic acid esters;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In this study, twelve new hexahydropyrimidine-2,4-dione derivatives were synthesized and screened for their anticonvulsant activities. All the compounds (7a-l) which have 6-arylhexahydropyrimidine-2,4-dione and N,N-disubstituted dithiocarbamate structures were prepared by the reaction with appropriate 3-(2-chloroethyl)-6-arylhexahydropyrimidine-2,4-diones and the corresponding N,N-disubstituted dithiocarbamate potassium salts. The structure of the synthesized compounds was confirmed by UV, IR, (1)H-NMR and elemental analysis. Their anticonvulsant activities were determined by maximal electroshock (MES), subcutaneous pentetrazol (metrazol, scMet) and rotorod toxicity tests for neurological deficits. According to the activity studies, 6(4-chlorophenyl)hexahydropyrimidine-2,4-dione derivatives (7e-h) were found to be highly protective against MES and scMet. Neurotoxicity was not observed in any of the tested compounds.
引用
收藏
页码:259 / 264
页数:6
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