In order to find novel pesticide leading compound with high bioactivity, ten bis-β-carboline derivatives linked by benzimidazole were synthesized starting from ethyl 1-substituted-β-carboline-3- carboxylate via alkylation, oxidation, and condensation. The structure of all novel compounds was confirmed by 1H NMR, 13C NMR and HRMS. Their antifungal activities were evaluated in vitro against five phytopathogenic fungi (Cotton Fusarium, Rhizoctonia solani, Sunflower sclerotinia, Rape sclerotinia, and Botrytis cinerea) using myvelium growth rate method. The preliminary results showed that most of the compounds possessed some fungicidal activity to five phytopathogenic fungi at 50 mg/L. These compounds have exhibited a significant inhibitory effect against sunflower sclerotinia rot in which compounds Ⅴb, and Ⅴi had inhibitory rates of 100%, and 92.4%, respectively. The information obtained from the studies may be useful for the design of novel agricultural fungicides.