A series of N-(thiazol-4-ylmethyl) benzenesulfonamide derivatives were designed, synthesized, and characterized by ¹H NMR, ¹³C NMR, and HRMS. The evaluation of fungicidal activities against Fusarium oxysporum (F. oxysporum), Sclerotinia sclerotiorum (S. sclerotiorum), Botrytis cinerea (B. cinerea), Colletotrichum fragariae (C. fragariae), Alternaria alternata (A. alternata), Penicillium digitatum (P. digitatum), Curvularia lunata (C. lunata), and Curvularia mebaldsii (C. mebaldsii) for the target compounds was carried out. The results indicated that this series of compounds were sensitive to C. lunata, B. cinerea, and S. sclerotiorum. Especially, 2,4-dichloro-N-((2-phenylthiazol-4-yl)methyl)benzenesulfonamide (5c) exhibited the best bioactivities against C. lunata, B. cinerea, and S. sclerotiorum with EC₅₀ value of 20.8 mg/L (52.3 μM), 24.6 mg/L (61.8 μM), and 9.5 mg/L (23.9 μM), respectively, which has equivalent or superior fungicidal activity to commercial products hymexazol. Furthermore, the structure–activity relationship was given, which might be contribution to the design and discovery of N-(thiazol-4-ylmethyl)benzenesulfonamide derivatives as novel fungicide.

设计、合成了一系列N- (噻唑-4-基甲基)苯磺酰胺衍生物，并通过¹ H NMR、¹³ C NMR和HRMS对其进行了表征。对尖孢镰刀菌（F. oxysporum）、核盘菌（S. sclerotiorum）、灰霉属（B. cinerea）、草莓炭疽菌（C. fragariae）、交替链格孢（A. alternata）、指状青霉（P . digitatum ), Curvularia lunata ( C. lunata) 和Curvularia mebaldsii ( C. mebaldsii ) 为目标化合物。结果表明，该系列化合物对C. lunata、B. cinerea和S. sclerotiorum均敏感。尤其是2,4-二氯-N -((2-苯基噻唑-4-基)甲基)苯磺酰胺( 5c )对C. lunata、B. cinerea和S. sclerotiorum的生物活性最好，EC ₅₀值分别为20.8 mg/L（52.3 μM）、24.6 mg/L（61.8 μM）和9.5 mg/L（23.9 μM），具有与市售产品恶霉灵相当或更高的杀菌活性。此外，还给出了构效关系，这可能有助于N- (thiazol-4-ylmethyl)苯磺酰胺衍生物作为新型杀菌剂的设计和发现。