posted on 2024-01-03, 09:05authored byXu Han, Renle Xu, Shihao Gu, Yue Kong, Yuhang Lou, Yanqing Gao, Shibin Shang, Zhanqian Song, Jie Song, Jian Li
To develop new antioomycete agents
against plant pathogens, two
series of acrylopimaric acid triazole derivatives from rosin were
synthesized. The in vitro antioomycete activity of
these derivatives was evaluated and screened against Pseudoperonospora cubensisi, Plasmopara
viticola, Phytophthora sojae, Phytophthora infestans, and Phytophthora capsici. Compound 5m showed
the highest antioomycete activity against P. capsici, with a half-maximal effective concentration (EC50) value
that was lower than that of the positive control metalaxyl (1.391
and 1.815 mg/L, respectively). Compound 5m demonstrated
satisfactory protective and curative efficacy against P. capsici in pepper in in vivo antioomycete
activity studies. Physiological and biochemical testing showed that
the action mechanism of compound 5m on P. capsici involved altering the morphology and ultrastructure
of the mycelium, increasing cell membrane permeability, inducing dysfunction
of the nucleus and mitochondria, and ultimately causing cell necrosis.
In addition, the analysis of three-dimensional quantitative structure–activity
relationship (3D-QSAR) revealed the significance of the molecular
structure and charge distribution in the interaction between compound 5m and its target. Collectively, these findings indicate that
compound 5m has the potential as an antioomycete candidate.