College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.
Molecules. 2020 Jul 31;25(15):3500. doi: 10.3390/molecules25153500.
To find pesticidal lead compounds with high activity, a series of novel benzamides substituted with pyridine-linked 1,2,4-oxadiazole were designed by bioisosterism, and synthesized easily via esterification, cyanation, cyclization and aminolysis reactions. The structures of the target compounds were confirmed by H-NMR, C-NMR and HRMS. The preliminary bioassay showed that most compounds had good larvicidal activities against mosquito larvae at 10 mg/L, especially compound , with a larvicidal activity as high as 100%, and even at 1 mg/L was still 40%; at 50 mg/L, all the target compounds showed good fungicidal activities against the eight tested fungi. Moreover, compound exhibited better inhibitory activity (90.5%) than fluxapyroxad (63.6%) against . Therefore, this type of compound can be further studied.
为了寻找具有高活性的杀农药用铅化合物，我们通过生物等排原理设计了一系列新型的吡啶连接的 1,2,4-恶二唑取代的苯甲酰胺，并通过酯化、氰化、环化和氨解反应很容易地进行了合成。目标化合物的结构通过 H-NMR、C-NMR 和 HRMS 得到了确认。初步的生物测定表明，大多数化合物在 10mg/L 时对蚊虫幼虫具有良好的杀虫活性，特别是化合物 ，杀虫活性高达 100%，甚至在 1mg/L 时仍有 40%；在 50mg/L 时，所有目标化合物对测试的 8 种真菌均表现出良好的杀菌活性。此外，化合物 对 的抑制活性（90.5%）优于氟环唑（63.6%）。因此，这种类型的化合物可以进一步研究。
