4-取代氨基-6-苯基嘧啶化合物的合成及抗惊活性  

Synthesis and Preliminary Study of the Anticonvulsant Activity of 4 Substituted Amino 6 Phenylpyrimidines

作　　者：张晓晖[1] 王东辉[1] 陈乃勇 陶成[1] 

机构地区：[1]北京医科大学药学院应用药物研究所,北京100083

出　　处：《中国药物化学杂志》1999年第3期192-195,共4页Chinese Journal of Medicinal Chemistry

摘　　要：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．On the basis of the anticonvulsive effect of cinnamamides and 3 alkyl 6 aryl 4(3 H ) pyrimidinones,fourteen compounds of 4 substituted amino 6 phenylpyrimidines(Ⅱ 1～Ⅱ 14 ) have been designed and synthesized.These compounds and their intermediate (Ⅲ) were tested in MES on mice.All the compounds were found to show some anticonvulsant activity.Among them,compounds (Ⅱ 9) and (Ⅱ 13 ) showed strong effects,even stronger than Dilantin sodium.We primarily imagined that the stereo constructure of the substituted groups on the N 4 atom could be a more important factor for activity.

关 键 词：苯基嘧啶 合成 抗惊活性 构效关系 

分 类 号：TQ463.54[化学工程—制药化工] R971[医药卫生—药品]