Abstract: The β-carboline derivatives were synthesized from indole formaldehyde and nitroethane via the Henry and Pictet-Spengler reaction.Twelve β-carboline derivatives were obtained and ten of them were new compounds.The structures of all the derivatives were confirmed by 1H NMR,13C NMR and ESI-MS.Antifungal activity test showed that compound Z-5 (9-isopropyl-3-methyl-β-carboline) has significant inhibitory activity against the spore germination of Curvularia lunata(Walker) Boedijn and Botrytis cinerea with EC50 value of 4.23 and 6.73 μg/mL.Compound Z-7 (3-methyl-9-propargyl-β-carboline) showed similarly antifungal activity as that of Z-5 with EC50 value of 11.16 and 7.51 μg/mL, respectively.