Survey on the Recent Advances in 4-Hydroxyphenylpyruvate Dioxygenase (HPPD) Inhibition by Diketone and Triketone Derivatives and Congeneric Compounds: Structural Analysis of HPPD/Inhibitor Complexes and Structure–Activity Relationship Considerations,Journal of Agricultural and Food Chemistry

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Survey on the Recent Advances in 4-Hydroxyphenylpyruvate Dioxygenase (HPPD) Inhibition by Diketone and Triketone Derivatives and Congeneric Compounds: Structural Analysis of HPPD/Inhibitor Complexes and Structure–Activity Relationship Considerations
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2022-06-02 , DOI: 10.1021/acs.jafc.2c02010
Paolo Governa ₁ , Giulia Bernardini ₁ , Daniela Braconi ₁ , Fabrizio Manetti ₁ , Annalisa Santucci ₁ , Elena Petricci ₁

Affiliation

The serendipitous discovery of the HPPD inhibitors from allelopathic plants opened the way for searching new and effective herbicidal agents by application of classical hit-to-lead optimization approaches. A plethora of active and selective compounds were discovered that belong to three major classes of cyclohexane-based triketones, pyrazole-based diketones, and diketonitriles. In addition, to enhance inhibitory constant and herbicidal activity, many efforts were also made to gain broader weed control, crop safety, and eventual agricultural applicability. Moreover, HPPD inhibitors emerged as therapeutic agents for inherited and metabolic human diseases as well as vector-selective insecticides in the control of hematophagous arthropods. Given the large set of experimental data available, structure–activity relationship analysis could be used to derive suggestions for next generation optimized compounds.

中文翻译：

二酮和三酮衍生物和同类化合物抑制 4-羟基苯丙酮酸双加氧酶 (HPPD) 的最新进展调查：HPPD/抑制剂复合物的结构分析和构效关系考虑

从化感植物中偶然发现 HPPD 抑制剂开辟了通过应用经典的先导优化方法寻找新的有效除草剂的途径。发现了大量的活性和选择性化合物，它们属于基于环己烷的三酮、基于吡唑的二酮和二酮腈三大类。此外，为了增强抑制恒定和除草活性，还做出了许多努力来获得更广泛的杂草控制、作物安全和最终的农业适用性。此外，HPPD 抑制剂已成为遗传性和代谢性人类疾病的治疗剂，以及控制食血节肢动物的载体选择性杀虫剂。鉴于可用的大量实验数据，

更新日期：2022-06-02

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