Study On Synthesis And Antifungal Activity Of Novel Triazole Compounds Containing Thiazideamide

Study on heterocyclic compounds with high bioactivity and low toxicity is a hotspot offungicide research, especially in the field of new fungicide development. To design andsynthesize various heterocyclic compounds is a significant way to obtain new compoundswith novel structure and high bioactivit.As heterocyclic compounds, triazole derivatives are widely studied for their structuralvariability, low poison and high activity. Thiazine, a six-membered ring containing nitrogenand sulfur atoms, has been widely applied in medical and pharmaceutical fields, rarely studiedin fungicides development. In order to create novel and efficient triazole fungicides, this studycombined the active groups triazole, amide and thiazine according to substructure linkingmethod.25novel compounds were synthesized from α-triazole pinacolone by the Knoevenageland Biginelli reactions with different substituted benzaldehyde, thiourea and acyl chloride.The structures of these compounds were confirmed by IR,~1H-NMR, and MS.The preliminary antifungal activity test indicated that all of the synthesized compoundsshowed different inhibition on six tested plant pathogenic fungus(Cytospora Mandshurica,Botrytis cinerea, Fusarium graminearum, curvularia lunata.boed, Fusarium solani andFusarium oxysporum vasinfectum) at the concentration of100mg/L．3a and3b series hadbetter fungicidal activity than other compounds against Botrytis cinerea. The inhibition ratesof compound3a-3,3a-4,3a-5,3b-2,3b-3and3d-1against Botrytis cinerea were up to100%,the same as3a-5against Fusarium graminerum. The inhibition rate of3c-5against Fusariumsolani was82.0%.3a-4against Fusarium oxysporum vasinfectum and3a-5against Pyriculariagrisea was93.7%and100%respectively.