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Design, synthesis and screening of herbicidal activity for new phenyl pyrazole-based protoporphyrinogen oxidase-inhibitors (PPO) overcoming resistance issues
Pest Management Science ( IF 4.1 ) Pub Date : 2023-02-23 , DOI: 10.1002/ps.7425
Rebecca L Mattison 1 , Roland Beffa 1 , Guido Bojack 1 , Birgit Bollenbach-Wahl 1 , Christine Dörnbrack 1 , Nicole Dorn 1 , Jörg Freigang 1 , Elmar Gatzweiler 1 , Rahel Getachew 1 , Claudia Hartfiel 1 , Ines Heinemann 1 , Hendrik Helmke 1 , Sabine Hohmann 1 , Harald Jakobi 1 , Gudrun Lange 1 , Peter Lümmen 1 , Lothar Willms 1 , Jens Frackenpohl 1
Affiliation  

Whilst there are several methods to control weeds, which continuously plague farmers around the globe, the application of small molecular compounds is still the most effective technology to date. Plants can evolve to become resistant to PPO-inhibitors, a class of herbicides in commercial use since the 1960s. It is therefore essential to continuously develop new herbicides based on this mode-of-action with enhanced intrinsic activity, an improved resistance profile and favourable physicochemical properties. Based on an Amaranthus PPO crystal structure and subsequent modelling studies, halogen-substituted pyrazoles have been investigated as isosteres of uracil-based PPO-inhibitors.

中文翻译:

新型苯基吡唑基原卟啉原氧化酶抑制剂 (PPO) 克服耐药性问题的设计、合成和除草活性筛选

虽然有多种方法可以控制不断困扰全球农民的杂草,但小分子化合物的应用仍然是迄今为止最有效的技术。植物可以进化为对 PPO 抑制剂产生抗性,PPO 抑制剂是 1960 年代以来商业使用的一类除草剂。因此,有必要根据这种作用方式不断开发新的除草剂,这些除草剂具有增强的内在活性、改进的抗性特征和良好的理化特性。基于苋属 PPO 晶体结构和随后的建模研究,卤素取代的吡唑已被研究为基于尿嘧啶的 PPO 抑制剂的等排物。
更新日期:2023-02-23
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