ALS酶抑制剂的设计合成及生物活性研究(X)磺酰脲和三唑并嘧啶磺酰胺除草剂的定量构效关系研究

DESIGN,SYNTHESES AND BIOLOGICAL ACTIVITY OF NOVEL HERBICIDES TARGETED ALS (X)QUANTITATIVE STRUCTURE ACTIVITY RELATIONSHIPS OF SULFONYLUREA AND TRIAZOLOPYRIMIDINE SULFONAMIDE HERBICIDES

摘要: 利用 Hansch方法定量地研究了 2 0种磺酰脲和 16种嘧啶磺酰胺除草剂的结构与活性间关系。结果表明这两类化合物的构效关系是一致的 ,这意味着它们能作用于靶标的同一部位。影响化合物活性的主要因素是分子的电性 ,它们与受体作用时具有一个最佳电性值 (Σσ或 p Ka)。

Abstract: The quantitative relationship between the structure of 20 sulfonylureas and 16 sulfonamides and their herbicidal activity against rape were analyzed using Hansch approach. The results showed that the structure activity relationships of the two sets of compounds were identical, which suggested that they might act on the same target site. The electronic properties of the molecules are dominant factor to the activity and there is apparently an optimum electronic property (Σσ or pKa) for the molecules to fit the receptor.