含硫醚结构的嘧啶磺酸酯类化合物的设计、合成与生物活性。
Design, Synthesis and Bioactivity of Novel Pyrimidine Sulfonate Esters Containing Thioether Moiety.
机构信息
Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, China.
出版信息
Int J Mol Sci. 2023 Feb 28;24(5):4691. doi: 10.3390/ijms24054691.
Pesticides play an important role in crop disease and pest control. However, their irrational use leads to the emergence of drug resistance. Therefore, it is necessary to search for new pesticide-lead compounds with new structures. We designed and synthesized 33 novel pyrimidine derivatives containing sulfonate groups and evaluated their antibacterial and insecticidal activities. Results: Most of the synthesized compounds showed good antibacterial activity against pv. (), pv. (), pv. () and (Rs), and certain insecticidal activity. , and showed strong antibacterial activity against , with EC values of 4.24, 6.77 and 9.35 μg/mL, respectively. Compounds , , and showed remarkable activity against (EC was 79.02, 82.28, 70.80 and 44.11 μg/mL, respectively). In addition, could significantly improve the defense enzyme (superoxide dismutase, peroxidase, phenylalanine ammonia-lyase and catalase) activity of plants against pathogens and thus improve the disease resistance of plants. Moreover, a few compounds also showed good insecticidal activity against and . The results of this study provide insight into the development of new broad-spectrum pesticides.
农药在作物病虫害防治中起着重要作用。然而，它们的不合理使用导致了抗药性的出现。因此，有必要寻找具有新结构的新农药先导化合物。我们设计并合成了 33 种含有磺酸基的新型嘧啶衍生物，并评估了它们的抗菌和杀虫活性。结果：大多数合成化合物对 pv. ()、pv. ()、pv. () 和 (Rs) 表现出良好的抗菌活性，并且具有一定的杀虫活性。 、 和 对 表现出很强的抗菌活性，EC 值分别为 4.24、6.77 和 9.35μg/mL。化合物 、 、 和 对 表现出显著的活性（EC 值分别为 79.02、82.28、70.80 和 44.11μg/mL）。此外， 可显著提高植物对病原体的防御酶（超氧化物歧化酶、过氧化物酶、苯丙氨酸解氨酶和过氧化氢酶）活性，从而提高植物的抗病性。此外，一些化合物对 和 也表现出良好的杀虫活性。本研究结果为开发新型广谱农药提供了思路。
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