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，为了增大γ－氨基丁酸的脂溶性，使其能透过血脑屏障进入脑组织，作者选用具有较高亲脂性的2，4－二羟基苯甲醛作为γ－氨基丁酸的亲脂性载体，设计并合成了6个4－（2，4－二羟基苯亚甲氨基）丁酸酯类化合物作为抗癫痫化合物进行抗惊厥活性实验，所合成的化合物均未见文献报道合成的样品经元素分析，红外光谱和核磁共振氢谱检测。
γ-aminobutyric acid (GABA) is a major inhibitory transmitter in the central nervous systcm of animals and mammalian. Most studies indicated that GANA plays a role in the pathophysiology of epilepsy. GABA increases the threshold of convulsion when it was adiministered locally in the brain of dog. Under physiologlcal condition GANA poorly crosses the blood-brain barrier, so it is not effective when administered orally. it is likely that a nontoxic GABA mimetic which easily enters the brain will have useful therapeutic properties. With this in mind, we have designed and synthesired 6 derivatives of γ-aminobutyric acid with an imine link (Schiff base) to a lipophilc carrier in order to facilitate the passage of γ-aminobutyric acid across the blood-brain barrier (Compounds 1, 2, 3, 4, 5, 6).The synthesised 6 target compounds were identified with elemental analysis, IR spectra and 1H-NMR spectra. it shows that the results were consistent with the proposed smicture.
出处
《贵州科学》
1998年第2期81-85,共5页
Guizhou Science
关键词
氨基丁酸
衍生物
合成
抗癫痫化合物
γ-aminobutyric acid derivatives, anticonvulsant activity, Synthesis
