Synthesis Of A Series Of Maleimide With Aminocyclitoland Comparion Of Their Antimicrobial Activities

Plant diseases caused by plant pathogenic fungi have resulted in large harm to the agriculture in every country.Sclerotinia sclerotioruM?Rhizoctonia solani and Botrytis cinerea,as two representatives of plant pathogenic fungi with a wide host range,complex origins,latent infection and strong saprophytism,are high-risk plant pathogen.Unfortunately,as the extensive use of the present fungicides,these pathogens exert resistance in some degree.In this case,developing novel,highly effective and structurally concise antifungal agents with low toxicities is an urgently challenging and especially significant task to control crop diseases.In the previous study,it has been reported that natural products with maleic anhydride structure or maleimide structure have high biological activities,but there are few species of natural maleimides.What's more,we have obtained validamine,valienamine,valiolamine and other aminocyclitol by biological degradation from the natural compound of validamycin,which also have excellent biological activity.Based on these compunds,seventeen new maleimides linked with aminocyclitol,were synthesized by methanol solution of sodium methoxide,and characterized by 1H NMR and MS.It is hopeful that can find out one or more new compounds,which may inhibit the world pathogents.The in-vitro antifungal activities studies against Sclerotinia sclerotiorum?Rhizoctonia solani and B.cinerea were preliminary investigated by the mycelium growth rate method.The results showed that the new of maleimides had no obviously inhibition on Sclerotinia sclerotiorum,Rhizoctonia solani and B.cinerea,but we expanded the compound library.Howereve,we found 2 of 17 compounds had interesting inhibitory with S.sclerotiorum.It provided a theoretical of a new antimicrobial.The innovation of this paper was combinated maleimides with aminocyclitol,both of them were natural compounds,which we hoped to get a new antimicrobial compounds.