jf8b02124_si_001.pdf (598.02 kB)
Discovery of β‑Carboline Oxadiazole Derivatives as Fungicidal Agents against Rice Sheath Blight
journal contribution
posted on 2018-08-22, 00:00 authored by Zhi-Jun Zhang, Zhi-Yan Jiang, Qi Zhu, Guo-Hua ZhongA series of β-carboline oxadiazoles
were synthesized, and their fungicidal activities and mechanism of
action against rice sheath blight caused by Rhizoctonia
solani was evaluated. The results showed that all
of these compounds exhibited significant in vitro fungicidal activity. Significantly, compound 5i (EC50 = 4.2 μg/mL) displayed the best efficacy and superior
fungicidal activity compared to validamycin A (EC50 = 197.6
μg/mL). Moreover, the in vivo test also demonstrated
that compound 5i could effectively control rice sheath
blight and showed higher in vivo protective and curative
activities against R. solani than validamycin
A. Preliminary mechanism studies revealed that compound 5i caused the loss of mitochondrial membrane potential, reactive oxygen
species accumulation, cell membrane destruction, and DNA synthesis
interference. These findings indicated that compound 5i displayed superior fungicidal activities against R. solani and could be a potential fungicidal candidate
against rice sheath blight.