Abstract
A series of saccharin derivatives containing 2-aminothiazole scaffold were designed,synthesized,and characterized by 1H NMR,~(13)C NMR,and HRMS.The fungicidal activities of these novel compounds against Botrytis cinerea,Curvularia lunata,and Rhizoctonia solani were evaluated.The results indicated that N-(4-((1,1-dioxido-3-oxobenzo[d]isothiazol-2(3H)-yl)methyl)thiazol-2-yl)acrylamide(HST3)displayed potential fungicidal activities against C.lunata,and R.solani with IC_(50)values of 15.0 mg/L and 12.9 mg/L respectively,which possessed higher fungicidal activity than commercial products hymexazol and amicarthiazol.Moreover,N-(4-((1,1-dioxido-3-oxobenzo[d]isothiazol-2(3H)-yl)methyl)thiazol-2-yl)-4-methoxybenzamide(HST9)possessed an IC_(50)value of 1.1 mg/L against B.cinerea,superior to hymexazol,amicarthiazol,and carboxin.Besides,the superficial structure-activity relationship was discussed.Furthermore,molecular docking result suggest that SDH enzyme might be one of the action targets of title compounds.
NSTL