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设计,合成和生物活性评估含有异环的单和双酸化合物

Xin Wu¹, Zili Yang¹, Mengwei Bu¹

¹National Key Laboratory of Green Pesticide, College of Chemistry, Central China Normal University, Wuhan 430079, China.

Molecules (Basel, Switzerland)

|November 25, 2023

概括

新的福斯米多辛 (FOS) 类似物与皮拉和异醇组显示出增强的除草剂活性. 这些化合物向2-C-甲基-D-氨酸4-酸盐 (MEP) 途径,为开发新型除草剂提供了有前途的战略.

科学领域:

药用化学医学化学
农业化学品农业化学品农业化学品
有机合成有机合成

背景情况:

胺 (FOS) 是一种天然化合物,在2-C-甲基-D-氨酸4-酸盐 (MEP) 途径中抑制1-deoxy-D-xylulose 5-phosphate降解异构酶 (DXR) 酶.
通过修改FOS结构来开发新的活性化合物是新药发现的可行策略.

研究的目的:

通过将胺酸单元替换为像pyrazole和isoxazole这样的异环体来设计和合成新型胺酸 (FOS) 类似物.
为了评估这些FOS类似物在各种植物物种上的除草剂活性.

主要方法:

FOS类型的合成涉及迈克尔加法和循环凝结反应.
生物活性评估包括在模型植物上出现前和出现后的除草剂活性测试.
进行了DXR抑制活性和二甲基亚酸救援试验.

主要成果:

与FOS相比,一些合成的FOS类似物表现出更高的除草剂活性.
最强效的类似物显示出对Arabidopsis thaliana,Brassica napus L.和Echinochloa crus-galli.的显著抑制.
尽管具有很高的除草剂活性,但一些类似物显示出较低的DXR抑制,这表明了其他作用机制.

结论:

在FOS中用异循环替代酸盐单元的生物异构替代是一种有效的策略,用于发现强大的除草剂化合物.
新型的FOS类似物代表了开发针对MEP途径或其他生物标的新农业化学品的有希望的候选者.

关键词:

DXRDXRDXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD DXRD 双酸是双酸中的一种.它具有除草剂活性.不同环的异环环.单酸单酸是一种酸.

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