Synthesis and Antifungal Activity of Some 6-tert-butyl-8-chloro-2, 3-dimethylquinolin-4-ol Derivatives against Pyricularia oryae

Background: A series of new 6-(tert-butyl)-8-chloro-2,3-dimethyl quinoline derivatives were designed and synthesized. Results: The primarily antifungal assay results indicated that all of them exhibited excellent protective efficacy (100%) against Pyricularia oryae at 100 ppm, except compound 2m (90%). Among them, the compound 2p (6-(tert-butyl)-8-chloro-2,3-dimethylquinolin-4-yl(2-chloro-5- (trifluoromethyl)benzyl)carbonate) possessed the highest fungicidal efficacy against Pyricularia oryae, even at 10 ppm. Conclusion: The structure-activity relationship showed that when the 2-position of benzene ring was substituted by F or Cl, the compound possessed good antifungal activity against Pyricularia oryae.