State Key Laboratory for Conservation and Utilization of Subtropical Agro-Bioresources, South China Agricultural University, Guangzhou, Guangdong 510642, China.
Key Laboratory of Natural Pesticide and Chemical Biology, Ministry of Education, South China Agricultural University, Guangzhou 510642, China.
J Agric Food Chem. 2021 Jun 2;69(21):5798-5803. doi: 10.1021/acs.jafc.0c04194. Epub 2021 May 24.
Sulfur(VI) fluorine exchange click reaction was applied to the highly efficient synthesis of new ,'-disubstituted sulfamide (RNH-SO-NHR) derivatives as pesticide candidates. Bioassays were conducted to evaluate both insecticidal and fungicidal activities of the target compounds. Preliminary results showed that the target molecules exhibited good bioactivities. In particular, insecticidal activities of compounds and against (LC = 2.42 and 3.87 μg·mL) were superior or adequate to that of commercial insecticide indoxacarb (LC = 3.99 μg·mL). Moreover, some compounds could also exhibit satisfactory fungicidal activity toward plant pathogens , , and . This work could bring new insights into the application of heterocyclic ,'-disubstituted sulfamides as novel pesticides.
硫（VI）氟代 click 反应被应用于新型，'-取代磺酰胺（RNH-SO-NHR）衍生物作为候选农药的高效合成。通过生物测定评估了目标化合物的杀虫和杀菌活性。初步结果表明，目标分子表现出良好的生物活性。特别是化合物和对 （LC = 2.42 和 3.87 μg·mL）的杀虫活性优于或相当于商业杀虫剂茚虫威（LC = 3.99 μg·mL）。此外，一些化合物对植物病原菌、和也表现出令人满意的杀菌活性。这项工作为杂环，'-取代磺酰胺作为新型农药的应用提供了新的思路。
