| Popis: |
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 |
Plný text