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（4’—氯苯基）（5—氟—2—羟基苯基）甲酮作为γ—氨基丁酸的亲脂性载体，设计并合成了7个4-[（4’—氯苯基）（5—氯—2—羟基苯基）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，所合成的化合物未见文献报道．合成的样品经元素分析、红外光谱和核磁共振氢谱检测，证实合成的化合物的结构与目标化合物一致．
γ- Aminobtuyric acid (GABA ) is a maior inhibitory transmitter in the central nervous system of animals and man. Most studies indicated that GABA plays a role in the pathophysiology of epilepsy. GABA increase the threshold of convulsion when it was adiminstered locally in the brain of dog. Under physiological conditon GABA poorly crosses the bloodbrain barrier, so it is not effective when adiministered 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 synthesized 7 derivatives of γ-aminobutyroc acid with an imine link (Schiff basc ) to a lipophilc carrier in order to facilitate the passage of γ-aminobutyric acid across the blood -brain barrier (compounds Ⅰ Ⅱ Ⅲ Ⅳ Ⅴ Ⅵ -Ⅶ ). The synthesized 7 title compound were identifide with elementary analysis and IR spectra. To confirm the structure of the compotinds, We deteminde the compounds Ⅰ Ⅱ Ⅲ Ⅳ Ⅴ Ⅵ -Ⅶ by 1HNMR spectra, TMS its internal standard. It shows that the results wers consistent with the proposed structure.
出处
《贵州大学学报（自然科学版）》
1998年第3期173-177,共5页
Journal of Guizhou University:Natural Sciences
