桂皮酰胺类化合物抗惊作用定量构效关系的研究

研究了38个杜皮酰胺类化合物的抗惊作用(MES)的定量构效关系。相关分析结果表明这类化合物的抗惊活性与脂水分配系数(logP正辛醇/水)呈抛物线的关系。苯环上取代基的Hammett σ常数和立体参数(MR)可以明显改进相关关系。说明吸电子同时体积小的取代基可以提高这类化合物的抗惊活性。使用上系列化合物中20个桂皮酰哌啶化合物研究定量构效关系,得到相似的结果。

QUANTITATIVE STRUCTURE-ANTICONVULSANT ACTIVITY RELATIONSHIPS OF CINNAMAMIDES

The anticonvulsant activities of thirty-eight cinnamamides have been used to formulate quantitative structure-activity relationships. The correlations indicate that the activity of these series of compounds is parabolically related to the partition coefficients (log P octanol/water) of the compounds. Hammett σ constants and steric parameter (MR) of the substituents can significantly improve the correlations. The equation indicates that the substituents with electron Withdrawing effect and small steric parameter will increase anticonvulsant activity of cinnamamide. The correlation analysis of twenty N-cinnamoyl piperidines out of the thirty-eight cinnamamides gives a similar equation.