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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
设计,合成和生物评估的新的马特林氧化埃斯特衍生物
Yan Li1, Kelin Li2, Xiaoping Zheng1
1State Key Laboratory for Development and Utilization of Forest Food Resources, Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, International Innovation Center for Forest Chemicals and Materials, Jiangsu Province Key Laboratory of Green Biomass Based Fuels and Chemicals, College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China.
合成了新型的马林衍生物,并对植物真菌进行了测试. 化合物5-11对Sclerotinia sclerotiorum表现出强烈的抗真菌活性,为农业提供了一个有前途的新型真菌杀菌剂.
科学领域:
- 农业科学 农业科学
- 菌类学 菌类学是指菌类学.
- 有机化学 有机化学
背景情况:
- 植物病原菌对全球农业构成重大威胁.
- 开发有效的低毒性杀菌剂对于作物保护至关重要.
研究的目的:
- 为了合成新型的oxime ester衍生物的matrine.
- 为了评估这些衍生品对常见的植物病原菌的抗真菌功效.
主要方法:
- 合成26种母体衍生物.
- 在体外抗真菌测试对七种植物病原菌进行了测试.
- 分子对接和动力学模拟以阐明作用机制.
主要成果:
- 化合物5-11在体外表现出显著的针对Sclerotinia sclerotiorum的活性 (EC50:7.2μg/mL),表现优于阿佐克西斯特罗宾.
- 化合物5-11对Sclerotinia sclerotiorum hyphae.表现出破坏性的影响.
- 分子模拟表明抑制酸脱酶 (SDH) 是可能的机制.
结论:
- 马特林衍生物,特别是5-11化合物,显示出作为新型农业杀菌剂的潜力.
- 化合物5-11的有效性可能与SDH抑制有关.
- 这项研究为开发以母为基础的植物保护剂提供了基础.
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