Lisciani R, Lembo S, Cozzolino S, La Rotonda M I, Silipo C, Vittoria A
Farmaco Sci. 1986 Feb;41(2):89-102.
A set of 2-aminobenzamide derivatives designed as analgesic following the principles of correlation analysis have been prepared and tested. The analgesic effects shown by these products are similar to those of non-narcotic analgesic drugs; moreover, they do not show antipyretic effects and are inactive or very poor inhibitors of prostaglandin synthesis. Quantitative structure-activity relationships (QSAR) show that the analgesic potency (writhing test) is a function of the octanol-water partition coefficient. The predictive value of a correlation equation previously published is clearly demonstrated.
按照相关分析原理设计的一组2-氨基苯甲酰胺衍生物已制备并进行了测试,这些衍生物用作镇痛药。这些产品显示出的镇痛效果与非麻醉性镇痛药相似;此外,它们没有解热作用,并且对前列腺素合成无活性或抑制作用非常弱。定量构效关系(QSAR)表明,镇痛效力(扭体试验)是正辛醇-水分配系数的函数。先前发表的相关方程的预测价值得到了明确证明。