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  • Title: Synthesis and in vivo fungicidal activity of some new quinoline derivatives against rice blast.
    Author: Liu XH, Fang YM, Xie F, Zhang RR, Shen ZH, Tan CX, Weng JQ, Xu TM, Huang HY.
    Journal: Pest Manag Sci; 2017 Sep; 73(9):1900-1907. PubMed ID: 28218818.
    Abstract:
    BACKGROUND: Quinoline derivatives possess excellent fungicidal activity against rice blast, but quinoline derivatives have not been thoroughly explored as fungicides. In the process of designing new fungicides, the 1,1,1,2,3,3,3-heptafluoropropan-2-yl group was introduced in order to find new structure quinoline derivatives. RESULTS: Seventeen new quinoline derivatives containing 1,1,1,2,3,3,3-heptafluoropropan-2-yl moiety were designed and synthesised. In vivo fungicidal activities of these compounds were tested against rice blast. Some of the compounds provided effective control at 100 mg L-1 , and a few compounds were effective at 10 mg L-1 . Furthermore, a density functional theory study established the structure-activity relationships of the synthesised compounds. CONCLUSION: Quinoline derivatives, especially benzyl (2,3,8-trimethyl-6-(perfluoropropan-2-yl)quinolin-4-yl) carbonate, which possess good control effective against rice blast and cucumber powdery mildew, may become new lead compounds for the development of fungicides with further structure modification. © 2017 Society of Chemical Industry.
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