噻二嗪磺酰胺类化合物的合成及其抑菌活性OA

To discover novel fungicide molecules with unique structures and excellent bioactivities,chesulfamide was employed as the lead compound,and a thiadiazine ring was introduced to design and synthesize a series of novel thiadiazine sulfonamide derivatives.The fungicidal activities of the target compounds were subsequently evaluated.The results demonstrated that at a concentration of 50 μg/mL,the target compounds exerted a certain inhibitory effect on five tested plant pathogens.Bioassay results indicated that seven compounds achieved inhibition rates exceeding 90%against Sclerotinia sclerotiorum.Specifically,compound C18 showed a 100.00%inhibition rate with an EC50 value of 0.06 μg/mL,which is superior to chesulfamide(1.12 μg/mL)and comparable to carbendazim and procymidone(0.05 μg/mL).Three compounds displayed inhibition rates over 70%against Botrytis cinerea,among which compound C12 reached an inhibition rate of 79.60%with an EC50 value of 8.16 μg/mL.In vivo control efficacy assay demonstrated that at 200 μg/mL,compounds C7,C18 and C23 exhibited control efficacies over 80%against Sclerotinia sclerotiorum,and compounds C7,C9,C13 and C15 showed control efficacies no less than 80%against Botrytis cinerea.This study provides a reference for the development of thiadiazine sulfonamide fungicides.