College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.
School of Environmental Science and Engineering, Suzhou University of Science and Technology, Suzhou 215009, China.
Molecules. 2022 Jul 22;27(15):4692. doi: 10.3390/molecules27154692.
In order to discover pesticidal lead compounds with high activity and low toxicity, a series of novel benzamides substituted with pyrazole-linked 1,2,4-oxadiazole were designed via bioisosterism. The chemical structures of the target compounds were confirmed via H NMR, C NMR and HRMS analysis. The preliminary bioassay showed that most compounds exhibited good lethal activities against , , and at 500 mg/L. Particularly in the case of , compound (70%) exhibited obvious insecticidal activity. In addition, compound demonstrated good fungicidal activity against with an inhibition rate of 77.8%, and compounds , , and also showed certain antifungal activities (55.6-66.7%). The zebrafish toxicity test showed that the LC of compound was 14.01 mg/L, which indicated that it may be used as a potential leading compound for further structural optimization.
为了发现具有高活性和低毒性的杀农药先导化合物，通过生物等排原理设计了一系列新型的吡唑连接 1,2,4-噁二唑取代的苯甲酰胺。通过 1 H NMR、13 C NMR 和 HRMS 分析确证了目标化合物的化学结构。初步的生物测定表明，大多数化合物在 500mg/L 时对 、 、 、 表现出良好的致死活性。特别是在 方面，化合物 （70%）表现出明显的杀虫活性。此外，化合物 对 表现出良好的杀菌活性，抑制率为 77.8%，化合物 、 、 也表现出一定的抗真菌活性（55.6-66.7%）。斑马鱼毒性试验表明，化合物 的 LC 为 14.01mg/L，这表明它可能被用作进一步结构优化的潜在先导化合物。
