香兰素(Vanillin,Ⅰ)是一种新型的抗癫癎物,经临床应用表明,可治疗各型癫癎,尤其适用于小发作,总有效率为86.1％,现已鉴定作为上市新药。经研究发现4-(2-羟乙基)香兰素Ⅱ)亦有抗惊作用,且毒性较小。我们对Ⅱ进行了结构改造并探讨了结构和活性间的量变关系。本文通过实验测定了羟乙基香兰素类化合物的los P,并用Leo碎片法和Hansch-Fujita π加合法进行了计算,取得了一致的结果。 Vanillin (Ⅰ) is a new type of anti-epileptic drug. It has been proved by clinical application that it can treat all kinds of epilepsy, especially for small ones. The total effective rate is 86.1%. It has been identified as a new drug for listing. The study found that 4- (2-hydroxyethyl) vanillin Ⅱ) also has anti-shock effect, and less toxic. We have carried out the structural transformation of Ⅱ and discussed the quantitative relationship between structure and activity. In this paper, los P of hydroxyethyl vanillin was determined experimentally and calculated by Leo fragmentation method and Hansch-Fujita π addition method. The results were consistent.