Synthesis of 1,2,3-triazole hydrazide derivatives exhibiting anti-phytopathogenic activity

Abstract

A series of new 1,2,3-triazole derivatives have been prepared and screened for their antifungal activity against phytopathogenic fungi using the mycelium growth inhibition method in vitro. The results indicated that the 1,2,3-triazole hydrazide scaffold displayed significant antifungal activity. Compound 6ad exhibited the most potent anti-phytopathogenic activity, with EC₅₀ values of 0.18, 0.35, 0.37 and 2.25 μg mL^-1 against Rhizoctonia solani, Sclerotinia sclerotiorum, Fusarium graminearum, and Magnaporthe oryzae, respectively. In vivo testing demonstrated that 6ad was effective for the control of rice sheath blight, rape sclerotinia rot, fusarium head blight and rice blast caused by the aforementioned phytopathogens. This work suggests that the combination of 1,2,3-triazole and hydrazide moiety could be a promising fungicide scaffold in the future.

Keywords: 1,2,3-Triazole; Antifungal activity; Fungicide; Hydrazide.