Abstract:In an attempt to search for natural product-based antifungal agents, α-campholenic aldehyde (III) was prepared by epoxidation and catalytic isomerization of α-pinene (I), and then converted into -campholenic (IV) acid and its acylchloride (V). Eight novel N-(4-(N-substituted sulfamoyl) phenyl)-α-campholenamide Ⅵa~Ⅵh were synthesized by N-acylation reaction of the acylchloride with various 4-amino-N-substituted benzenesulfonamide in 32.8~78.1% yield. All the target compounds were characterized by FTIR, 1HNMR, 13CNMR and ESI-MS. Antifungal activity test showed that, at the concentration of 50 µg/mL, all the target compounds exhibited a certain antifungal activity, in which compound N-[4-(N-(thiazol-2-yl)sulfamoyl)phenyl]-α-campholenamide(VIe) had inhibition ratio of 71.3% (B-class activity level) and 68.0% (C-class activity level) against Fusarium graminearum and Fusarium oxysporum f. cucumerinum, respectively.