[Synthesis of 4-[(4-chlorophenyl) (5-fluoro-2-hydroxyphenyl) methylene amino]butyrates and its anticonvulsant activity].
It is known that gamma-aminobutyric acid (GABA) plays an important role in the pathophysiology of epilepsy. Under physiological conditions it is very difficult for GABA to cross the blood-brain barrier. It is likely that the esters of GABA, Which easily enter the brain, will have useful therapeutic properties. With this in mind, we have designed and synthesized 8 derivatives (IVa to IVh) of gamma-aminobutyric acid with an imine to link a lipophilic carrier in order to facilitate the passage of gamma-aminobutyric acid to cross the blood-brain barrier. All the eight synthesized title compounds were evaluated as anticonvulsants in mice via the Antiepileptic Drug Development Program of NIH. The compounds IVb and IVf showed anticonvulsant activity.
Yuan
M
M
Zhong
Y
Y
Pang
Q
Q
Li
Z
Z
D000613:Aminobutyrates / Q000138:chemical synthesis* / Q000737:chemistry; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis*; D010636:Phenols / Q000138:chemical synthesis* / Q000737:chemistry
D000613:Aminobutyrates; D000927:Anticonvulsants; D010636:Phenols