摘要
γ－ 氨基丁酸在生理条件下不易透过血脑屏障进入脑组织，选用具有较高亲脂性的（５ － 氟－ ２－ 羟基苯基）（４′－ 氯苯基） 甲酮作为γ－ 氨基丁酸的亲脂性载体，设计并合成７ 个４ － ［（５ － 氟－ ２ － 羟基苯基）（４′－ 氯苯基） 亚甲氨基］ 丁酸酯类化合物作为抗癫痫化合物进行抗惊厥活性实验。经元素分析、红外光谱、质谱和核磁共振氢谱检测证实，合成的化合物结构与目标化合物一致。
Most studies indicated that GABA appears to play a role in the pathophysiology of epilepsy. Under physiological condition GABA poorly crosses the blood-brain barries, therefor it is not effective when administered orally. it is likely that a nontoxic γ-aminobutyric acid mimesis which easily enters the brain will have useful therapeutic properties. With this in mind, we have designed and synthesized seven 4[(5-fluro-2-hydroxyphenyl)(4-choropheny)methylene amino] butyrates, (Compounds ⅠⅡⅢⅣⅤⅥⅦ), in order to facilitate the passage of γ-aminobutyric acid across the blood-brain barrier. The synthesized 7 title compounds were identified with elemental analysis, IR Spectra,′H-NMR spectra and mass spectra.The results show that these compounds are consistent with chemical structure.
出处
《贵阳医学院学报》
CAS
1999年第4期342-346,共5页
Journal of Guiyang Medical College
关键词
氨基丁酸类
合成
抗惊厥活性
aminobutyric acid
synthesis
anticonvulsant activity
