贵州医科大学学报

1999, (04) 342-346

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4-[(5-氟-2-羟基苯基)(4′-氯苯基)亚甲氨基]丁酸酯类化合物的合成
Synthesis of 4-[(5-Fluro-2-Hydroxyphenyl) (4′-Choropheny)Methylene Amino] Butyrates

袁牧,钟裕国,庞其捷
Yuan Mu; et al Department of pharmacy;Guiyang Medical College;

摘要(Abstract):

 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.

关键词(KeyWords): 氨基丁酸类;合成;抗惊厥活性
aminobutyric acid; synthesis; anticonvulsant activity

Abstract:

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作者(Authors): 袁牧,钟裕国,庞其捷
Yuan Mu; et al Department of pharmacy;Guiyang Medical College;

DOI: 10.19367/j.cnki.1000-2707.1999.04.007

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