Synthesis and anticonvulsant activity of some potential thiazolidinonyl 2-oxo/thiobarbituric acids
Synthesis and anticonvulsant activity of some potential thiazolidinonyl 2-oxo/thiobarbituric acids
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DOI：
10.1016/j.ejmech.2006.03.029
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发表时间：
2006-10-01
影响因子：
6.7
通讯作者：
Kumar, A.
中科院分区：
文献类型：
--
作者：
Agarwal, A.;Lata, S.;Kumar, A.
通过5-肼基-2-氧代/硫代巴比妥酸(2a-2b)与各种芳香醛的缩合合成了一系列5-[(N-取代的亚苄基亚氨基)氨基]-2-氧代/硫代巴比妥酸(3a-3h)。巯基乙酸与3a-3h环加成，得到5-[(2'-取代的苯基-4'-氧代噻唑烷-3'-基)氨基]-2-氧代/硫代巴比妥酸(4a-4h)。所有这些化合物都经过体内筛选，以了解其抗惊厥活性和急性毒性研究。化合物 4f 和 4g 被发现是该系列中最有效的化合物，并与参考药物苯妥英钠、拉莫三嗪和丙戊酸钠进行了比较。这些化合物的结构已通过 IR、H-1 NMR 和质谱数据确定。 (c) 2006 年 Elsevier Masson SAS。版权所有。
A series of 5-[(N-substituted benzylidenylimino)amino]-2-oxo/thiobarbituric acids (3a-3h) have been synthesized by the condensation of 5-hydrazino-2-oxo/thiobarbituric acids (2a-2b) with various aromatic aldehydes. Cycloaddition of thioglycolic acid to 3a-3h, yielded 5-[(2'-substituted phenyl-4'-oxothiazolidin-3'-yl)amino]-2-oxo/thiobarbituric acids (4a-4h). All these compounds were screened, in vivo, for their anticonvulsant activity and acute toxicity studies. Compounds 4f and 4g were found to be most potent compounds of this series and were compared with the reference drugs, phenytoin sodium, lamotrigine and sodium valproate. The structures of these compounds have been established by IR, H-1 NMR and mass spectroscopic data. (c) 2006 Elsevier Masson SAS. All rights reserved.