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杀菌剂、除草剂和杀虫剂先导物的筛选规则。

Screening rules for leads of fungicides, herbicides, and insecticides.

机构信息

Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, China.

出版信息

J Agric Food Chem. 2010 Mar 10;58(5):2673-84. doi: 10.1021/jf902639x.

Abstract

To increase efficiency of finding leads in pesticide design, reasonable screening rules for leads of fungicide, herbicide, and insecticide, respectively, are desired. Previous works showed that "Rule 5" of Lipinski is not a suitable screening rule for leads of pesticide and proposed rules for leads of fungicide, insecticide, and herbicide, which were combined by logarithmic ratio of octanol-water partition coefficient (log P), number of hydrogen bond donors, molecular weight, number of hydrogen bond acceptors, polar surface area, carcinogenic toxicity, and mutagenic toxicity. Herein, three sets of screening rules for leads of fungicide, insecticide, and herbicide, respectively, are presented. Each set of screening rules involves seven descriptors, which were selected by Kolmogorov-Smirnov test, ANOVA, Kruskal-Wallis test, and Pearson product-moment correlation, from more than 450 descriptors calculated by Codessa. Their accuracies are about 82, 83, and 89%, respectively.

摘要

为了提高农药设计中先导化合物筛选的效率,人们期望分别为杀菌剂、除草剂和杀虫剂的先导化合物制定合理的筛选规则。先前的工作表明,里彭斯基(Lipinski)的“规则 5”不适用于农药先导化合物的筛选,并提出了杀菌剂、杀虫剂和除草剂先导化合物的规则,这些规则是通过辛醇-水分配系数(log P)、氢键供体数、分子量、氢键受体数、极性表面积、致癌毒性和致突变毒性的对数比来组合的。本文提出了三套杀菌剂、杀虫剂和除草剂先导化合物的筛选规则。每套筛选规则都涉及到七个描述符,这些描述符是通过柯尔莫哥洛夫-斯米尔诺夫检验(Kolmogorov-Smirnov test)、方差分析(ANOVA)、克鲁斯卡尔-沃利斯检验(Kruskal-Wallis test)和皮尔逊积矩相关系数(Pearson product-moment correlation),从 Codessa 计算的 450 多个描述符中选择出来的。它们的准确性分别约为 82%、83%和 89%。

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