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设计,合成和含碳胺杀菌剂的生物活性

Xiaocao Quan¹, Kunkun Shen¹, Wu-Lin Yang¹

¹Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.

Journal of agricultural and food chemistry

|July 26, 2024

概括

新型含的碳胺被合成并测试其抗真菌活性. 化合物3a表现出强大的糖酸脱酶抑制,表现优于博斯卡利德,并显示出作为新型真菌杀菌剂候选人的承诺.

科学领域:

农业化学农业化学
药用化学医学化学
有机合成有机合成

背景情况:

生物异构替代是设计用于作物保护的生物活性分子的关键策略.
碳胺是关键的化合物类别,在农业和医学中具有应用.

研究的目的:

为了合成含的新型碳胺.
评估它们的抗真菌和酸脱酶 (SDH) 抑制活性.
为了确定潜在的新SDHI用于作物保护.

主要方法:

合成了21种含的新型碳胺.
在体外测试抗真菌活性对关键的植物病原体.
酶分析以确定SDH抑制活性.
分子对接和扫描电子显微镜用于作用模式研究.

主要成果:

化合物3a,3e,4l和4o在体外表现出优异的抗真菌作用,对抗Rhizoctonia solani,Sclerotinia sclerotiorum,Botrytis cinerea和Fusarium graminearum. 这些化合物具有很好的抗真菌作用.
与博斯卡利德相比,化合物4l和4o对R. solani和S. sclerotiorum的EC50值更高.
化合物3a显示显著更高的SDH酶抑制活性 (IC50 = 8.70 mg/L) 比博斯卡利德 (IC50 = 22.09 mg/L).

结论:

新型含碳胺,特别是3a化合物,显示出作为酸脱酶抑制剂 (SDHI) 的显著潜力.
化合物3a表现出有前途的抗真菌活性和类似于Boscalid的作用方式.
对3a化合物进行进一步的研究是有必要的,以使其成为一种新的作物保护剂.

关键词:

博斯卡利德 (Boscalid) 是一个波斯卡利德.SDHIHI SDHI 的意思是 SDHI 的意思.生物异构体替代药物碳胺类杀菌剂是一种杀菌剂.含有的化合物含有的化合物结构结构活动关系关系

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