Studies On Synthesis And Antifungal Activities Of Analogues Based On Kakuol(â…£)

In the process of creating efficient, low toxicity, environmentally friendly pesticides,plant-based pesticides were paid more and more attention due to their extensive source,obtaining easily, low toxicity, environmentally friendly, low residue and catering for therequirement of the modem environmental protection and health. So it will become themainstream of the fungicide to find new active substances from the natural plant substancesor to be modeled after known natural products with activity and to explore thestructure-activity relationship, thereby increasing the level of activity. Pesticide research anddevelopment has became an important way of producing new pesticides.Kakuol is the main ingredient in the volatile oil of Asarum forbesii Maxim and hassignificant activity, because of its simple structure, great transformation and modificationpotential, it is possible to become a natural products model for pesticide synthesis research.This study combining the structural characteristics of kakuol and according to substructurelinking method,27imine derivatives were synthesized with sesamol as raw material. Thestructures of all the compounds were confirmed by IR,1H-NMR, and MS.The preliminary fungicidal activity results indicated that the27compounds showeddifferent inhibition against Fusarium solani, Botrytis cinerea, Alternaria alternata keissler,Alernaria sonali, Glomerella cingulata and Fusarium oxysporum vasinfectum at theconcentration of100mg/L. The compounds of4a and4b series exhibited better antifungalactivities than the compounds of4c series. The compounds containing chlorine atoms havebetter inhibitory effect against the fungi tested than most other compounds. The inhibitionrate of4a-5and4b-7against Altermaria sonali, Alternaria alternata keissler and Botrytiscinerea were all more than90%and higher than that of the positive control Azoxystrobin.