New Sulfone Compounds Antibacterial Activity Screening And Mechanism Of A Preliminary Study

As an important kind of compounds in pesticide field, sulfone derivatives have broad spectrum bioactivities, such as, pesticidal, antifungal, herbicidal, acaricidal activity. The application and development of sulfone derivatives have attracted a great deal of attention. We designed and synthesized a serial of heterocyclic sulfone compounds from Gallic acid which is one of important rescource in Guizhou Province. The studies disclosed that the compounds 05331 and 05338 showed remarkable inhibitory effect on 8 kinds of plant pathogenic fungus with the method of growth rate in lab. The EC₅₀ of 05331 and 05338 on B. cinerea, S. sclerotiorum, P. grisea, F. graminearum, C. gloeosporioides, R. solani, R. solani, P. infestan were 2.87 mg/L, 4.28 mg/L, 17.80 mg/L, 25.12 mg/L, 26.30 mg/L, 39.80 mg/L, 45.60 mg/L, 51.40mg/L and 11.74 mg/L, 12.50 mg/L, 30.82 mg/L, 28.84 mg/L, 21.83 mg/L, 90.74 mg/L, 93.33 mg/L, 83.18 mg/L, respectively.Gallic acid is one of important intermediates in pesticide field. A great deal of experiment results indicated that heterocyclic sulfone derivatives designed and synthesized from Gallic acid had significant inhibitory effect on plant pathogenic fungus. In order to supply reference for the structural optimization of sulfone derivatives and application in the development of the green fungicide, we studied the primary antifungal action mechanism of sulfone derivatives 05331 and 05338 with the teniques of morphology and enzymology. The results indicated that the highly effective sulfone antifungal compounds 05331 and 05338 could increase the permeability of cell membrane. The interference of membrane function would affect the content and activity of a series of biological molecules including soluble protein, reducing sugar, D-GluNAc and chitinase.