摘要：A series of novel 3,4-dichloroisothiazole based 1,2,4-triazole derivatives were rationally designed and synthesized. Their structures were confirmed by IH NMR, 13C NMR, HRMS or elemental analysis; the typical crystal structure was determined by X-ray diffraction for validation. All target compounds were evaluated for their in vitro fungicidal and in vivo anti-TMV activities. The bioassay results indicated that compound 6b, namely 1-（3,4-dichloroisothiazol-5-yo）-o-（4-ouorophenyo）-2-（OH-o,2o4-triazol-o-yl）ethanol, exhibited excellent growth inhibition against B. cinerea, C. arachldico;a and P. piricola with median effective concentrations （EC50） of 6.98, 2.73 and 3.07μg/mL, respectively, and good in vivo anti-TMV activity of over 60% of inactivation and induction activity at 100 μg/mL. These data demonstrate that compound 6b is both a fungicide and an anti-TMV lead, deserving further studies.

摘要：In searching for novel fungicidal leads,a series of pyrazole-containing strobilurins were rationally designed,synthesized and *** indicated that compound 1-7 displayed excellent fungicidal activity against a broad spectrum of plant pathogens such as Gibberella zeae,Rhizoctonia cereolis,Sclerotinia sclerotiorum,Phytophthora infestans,Physolosporo piricola and Pellicularia sosakii with EC_(50) of 0.16,0.02,0.72,0.07,0.77 and 0.65μg/mL,respectively,which were 3-10 times more potent than the positive control azoxystrobin against the corresponding ***,like azoxystrobin and kresoxim methyl,1-7,displayed excellent protec-tive activity against *** docking validated that 1-7 and azoxystrobin would share a similar binding mode with cytochrome bc_(1) *** study demonstrates that 1-7 is a promising fungicidal candidate for further development.