School of Science, Anhui Agricultural University, Hefei 230036, China.
College of Plant Protection, Northwest A&F University, Yangling 712100, China.
J Agric Food Chem. 2021 Sep 29;69(38):11395-11405. doi: 10.1021/acs.jafc.1c02454. Epub 2021 Sep 15.
Plant pathogenic fungi seriously threaten agricultural production. There is an urgent need to develop novel fungicides with low toxicity and high efficiency. In this study, we designed and synthesized 44 pyrazolo[3,4-]pyrimidin-4-one derivatives and evaluated them for their fungicidal activities. The bioassay data revealed that most of the target compounds possessed moderate to high in vitro antifungal activities. Especially compound exhibited remarkable antifungal activity against with an EC value of 1.25 mg/L, close to that of commercial fungicide (EC = 0.96 mg/L) and (EC = 1.91 mg/L). Moreover, compound possessed prominent protective activity against in vivo for 24 h (95.23%) and 48 h (93.78%), comparable to positive control (24 h (96.63%); 48 h (93.23%)). Subsequent studies indicated that compound may impede the growth and reproduction of by affecting the morphology of mycelium, destroying cell membrane integrity, and increasing cell membrane permeability. In addition, the application of compound did not injure the growth or reproduction of Italian bees. This study revealed that compound is expected to be developed for efficient and safe agricultural fungicides.
植物病原真菌严重威胁农业生产。因此，迫切需要开发低毒性、高效的新型杀菌剂。本研究设计并合成了 44 种吡唑并[3,4-d]嘧啶-4-酮衍生物，并评估了它们的杀菌活性。生物测定数据表明，大多数目标化合物具有中等至较强的体外抗真菌活性。特别是化合物 对 表现出显著的抗真菌活性，EC 值为 1.25mg/L，接近于商业杀菌剂 （EC = 0.96mg/L）和 （EC = 1.91mg/L）。此外，化合物 对 具有显著的体内保护活性，24 h（95.23%）和 48 h（93.78%），与阳性对照 （24 h（96.63%）；48 h（93.23%））相当。后续研究表明，化合物 可能通过影响菌丝形态、破坏细胞膜完整性和增加细胞膜通透性来阻碍 的生长和繁殖。此外，化合物 的应用不会损害意大利蜜蜂的生长或繁殖。本研究表明，化合物 有望开发为高效、安全的农业杀菌剂。
