β-取代桂皮酰胺类化合物的化学结构与抗惊活性的关系

为考查化学结构和抗惊活性之间的关系,设计并合成了一系列β位取代的桂皮酰胺化合物。发现其中有三个化合物(β位乙基、丙基、氨基取代物)抗惊活性较高。研究化学结构和抗惊活性的关系可看出:β位以给电子基团取代,并且苯环和羰基保持共轭体系的分子可增强抗惊活性。

Chemical structure-anticonvulsant activity relationship in beta-substituted cinnamamides

A series of β-substituted para-ch-lorocinnamamide compounds were designed for the study of the relationship between chemical structure and anticonvulsant activity. Three compounds (β-C₂H₅, β-C₃H₇,β-NH₂ substituted) were found to show higher activity.The relationships between chemical structure and anticonvulsant activity were discussed.1. Electron-repelling substituting groups are favourable to the anticonvulsant activity.2. The existence of resonance in the molecule seems essential for the anticonvulsant activity.