异噻唑啉酮类化合物的合成与生物活性.pdfVIP

第53卷第10期 农药 Vol.53, No.10 2014年10月 AGROCHEMICALS Oct. 2014 徐英, 张静, 李淼, 等. 异噻唑啉酮类化合物的合成与生物活性[J]. 农药, 2014, 53(10): 712-714. 异噻唑啉酮类化合物的合成与生物活性 徐 英，张 静，李 淼，周继中，王军锋，刘长令 (沈阳化工研究院有限公司新农药创制与开发国家重点实验室，沈阳11002 1) 摘要：[ 目的]发现具有较好生物活性的异噻唑啉酮类化合物。[方法] 以异噻唑啉酮类工业用杀菌剂为先导，利用 “中间体衍生方法 ，合成10个含异噻唑啉酮的二芳醚类化合物，并对其进行生物活性筛选。[结果]初步生物活 性数据表明 该类化合物在25 mg/L时对水稻稻瘟病和黄瓜灰霉病有一定的抑制作用。[结论]该类化合物可以作 为先导化合物进一步优化研究。 关键词：异噻唑啉酮；合成；杀菌活性 中图分类号：TQ460.3 文献标志码：A 文章编号：1006-04 13(20 14) 10-0712-03 Synthesis and Biological Activity of Isothiazolone Derivatives XU Ying, ZHANG Jing, LI Miao, ZHOU Ji-zhong, WANG Jun-feng, LIU Chang-ling (State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Co., Ltd., Shenyang 110021, China) [Aims] The study aims to discover some isothiazolone compounds with good bioactivity. [Methods] By method of intermediate derivatization method ten diaryl ether containing isothiazolone derivatives were synthesized and bioassayed employing some isothiazolone fungicides in industry as the lead compound. [Results] The preliminary biological activity tests showed that some of the title compounds had good activities to Pyricularia oryz ae and Pse udop eronosp ora cubens is at concentration 25 mg/L. [Conclusions] The isothiazolone compounds can be used as lead compounds for further optimization. isothiazolone; synthesis; fungicidal activity [5-6] 异噻唑啉酮类化合物是一类新型的高效广谱杀菌 污剂 。虽 异噻唑啉酮类化合物因具有良好的环境特 剂，具有高效、低毒、药效持续时间长、对环