γ-氨基丁酸衍生物的合成及抗惊厥活性

Synthesis and anticonvulsant activity of γ aminobutyric acid derivatives

目的：寻求具有抗惊厥活性，容易进入脑内的非毒性的γ氨基丁酸衍生物。方法：通过亚胺键将γ氨基丁酸接到一个亲脂性载体上，设计并合成了１６个γ氨基丁酸衍生物，测试其抗惊厥活性。结果：有６个化合物具有抗惊厥活性。结论：通过亚胺键将一个亲脂性载体接到γ氨基丁酸上制成的衍生物可能具有抗惊厥活性。

OBJECTIVE:To study nontoxic derivatives of γ aminobutyric acid which may easily enters the brain and have anticonvulsant activity.METHOD:16 derivatives of γ aminobutyric acid with an imine link to a lipophilic carrier were prepared and tested for anticonvulsant activity. RESULTS:6 compounds showed anticonvulsant activity.CONCLUSION:It indicated that a derivative of γ aminobutyric acid with an imine link to a lipophilic carrier may have useful anticonvulsant activity.