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设计合成了14 个4取代氨基6苯基嘧啶类化合物.小鼠MES抗惊实验结果表明:所合成的化合物及中间体( Ⅲ) 都有不同程度的抗惊活性,其中( Ⅱ9) 和( Ⅱ13) 抗惊活性最强,甚至超过对照品苯妥英钠.初步推测,4 位氨基氮原子上取代基的空间结构对抗惊活性有重要影响.
Design and synthesis of 14 4-substituted amino 6 phenyl pyrimidine compounds. The results of MES anticonvulsant assay showed that all of the synthesized compounds and intermediates (Ⅲ) had different degree of anti-shock activity, among them, (Ⅱ9) and (Ⅱ13) had the strongest anti-shock activity even more than the reference substance phenytoin sodium. It is preliminarily speculated that the spatial structure of the substituent on the 4-amino nitrogen atom has an important influence on the anti-shock activity.