摘要
作者设计并合成了9个Schiff碱型取代对羟基本甲醛缩r-氨基丁酸酯类化合物。并用美国NIH提出的“抗癫痫药物开发程序(ADD)对所合成的化合物进行抗惊厥活性筛选。结果表明化合物Ⅲf、Ⅲg、Ⅲh、Ⅲi具有不同程度的抗惊厥活性。
Most studies indica-
ted thai r-amino-butyric acid (GABA)
plays a role in the pathophysiology of
epilepsy. Under physiological conditions
GABA poorly crosses the blood-brain bar-
rier. It is likely that the ester of GABA
may easily enter the brain to increase the
therapeutic index, In addition to, the
vaniline processes the anticonvulsant acti-
vity, So that we have designed and synt-
hesized 9 schiff bases from subetituted p-
hydroxybenzaldehyde and the esters of
GABA (Ⅲ_a～Ⅲ_i). These Compounds
have not been reported, their Chemical
structurs have been Confirmed by IR.
NME. Ms and elemenlary analysis.
All the synthesized 9 title compounds
were evaluated at anticonvulsants in mice
via the antiepilelic drug development
Program of NIH. Compounds Ⅲ_f, Ⅲ_g,
Ⅲ_h, Ⅲ_i showed anticonvulsant activity.
出处
《华西药学杂志》
CAS
CSCD
北大核心
1990年第1期11-14,共4页
West China Journal of Pharmaceutical Sciences
关键词
氨基丁酸酯
合成
抗惊厥活性
derivative of r-Aminobutyric acid
Schiff bases of ester of GABA
Anticonvulant activity
