4-(4-羟基苯亚甲氨基)丁酸酯类衍生物的合成Synthesis of 4-[(4 -Hydrophenyl) Methylene Aminol Butyrates
袁牧;钟裕国;庞其捷;李正化;
Yuan Mu, et al Department of Pharmaceutical Chemistry
摘要(Abstract)：
作者以4-羟基苯甲醛作为Υ-氨基丁酸的亲脂性载体,设计并合成了3个4-(4-羟基苯亚甲氨基)丁酸酯类衍生物作为抗惊厥化合物供药理筛选。所合成的化合物尚未见文献报道。
Most studies have indicated that γ-aminobutyric acid (GABA) plays a role inthe pathophysiology of epilepsy GABA increase the threshold of convulsion when it was administered locally in the brain of dog.Under physiological condition GABA 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 synthesized 3 derivatives of γ-aminobutyric acid with an imine like (Schiff base) to a lipophilic carrier in order to facilitate that the passage of GABA across the blood-brain barrier (Ⅱa, Ⅱb, Ⅱc),These Compounds have not been reported, their chemical structure were primary identified with IR Spectra
关键词(KeyWords)：
γ-氨基丁酸衍生物;Schiff;碱型;γ-氨基丁酸酯
derivative of γ-aminobutyric acid;Schiff bases of γ-aminobutyrates
基金项目(Foundation):
作者(Author):
袁牧;钟裕国;庞其捷;李正化;
Yuan Mu, et al Department of Pharmaceutical Chemistry
Email:
DOI: 10.19367/j.cnki.1000-2707.1990.04.008
参考文献(References)：
- 1． Enna S J, et al. Biochemical pharmacology of GABAergic agonists Life Sci 1979; 24: 1727-1738．
- 2． A V Christensen and p Krogsgaard-Larsen. GABA Agonists: Molecular and Behavioural pharmacology. In: R G Fariello, et al. Neurotransmitters, Sei zures, and Epilepsy. New York: Raven Press 1984: 109-121．
- 3． Hayashi T. The inhibitory action of aminobutyric acid upon the seisure following stimulation of motor cortex of the dog.J Physiol 1959; 145: 570
- 4． Chase T N and Walters J R. In: Roberts E, et al.GABA in Nervous System Function. New York: Raven press, 1976: 497．
- 5． 钟裕国,等.天麻甙元同系物与同型物的合成及其中枢镇静抗惊活性.四川医学院学报 1984;15(1) :17-22．
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