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Discovery of Novel (5-Mercapto-4-phenyl-4H-1,2,4-triazol-3-yl)methyl Phenyl Carbamate as a Potent Phytoene Desaturase Inhibitor through Scaffold Hopping and Linker Modification.
Zhang, Di; Wang, Chunxue; Zhang, Yichi; Yu, Zhilei; Hong, Zeyu; Jia, Ding; Ma, Dejun; Gu, Yucheng; Xu, Han; Xi, Zhen.
Afiliación
  • Zhang D; National Pesticide Engineering Research Center (Tianjin), Department of Chemical Biology, State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, P. R. China.
  • Wang C; Frontiers Science Center for New Organic Matter, Nankai University, Tianjin 300071, P. R. China.
  • Zhang Y; National Pesticide Engineering Research Center (Tianjin), Department of Chemical Biology, State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, P. R. China.
  • Yu Z; Frontiers Science Center for New Organic Matter, Nankai University, Tianjin 300071, P. R. China.
  • Hong Z; National Pesticide Engineering Research Center (Tianjin), Department of Chemical Biology, State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, P. R. China.
  • Jia D; Frontiers Science Center for New Organic Matter, Nankai University, Tianjin 300071, P. R. China.
  • Ma D; National Pesticide Engineering Research Center (Tianjin), Department of Chemical Biology, State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, P. R. China.
  • Gu Y; Frontiers Science Center for New Organic Matter, Nankai University, Tianjin 300071, P. R. China.
  • Xu H; National Pesticide Engineering Research Center (Tianjin), Department of Chemical Biology, State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, P. R. China.
  • Xi Z; Frontiers Science Center for New Organic Matter, Nankai University, Tianjin 300071, P. R. China.
J Agric Food Chem ; 72(34): 18898-18908, 2024 Aug 28.
Article en En | MEDLINE | ID: mdl-39147603
ABSTRACT
Phytoene desaturase (PDS) is a key rate-limiting enzyme in the carotenoid biosynthesis pathway. Although commercial PDS inhibitors have been developed for decades, it remains necessary to develop novel PDS inhibitors with higher bioactivity. In this work, we used the scaffold hopping and linker modification approaches to design and synthesize a series of compounds (7a-7o, 8a-8l, and 14a-14d). The postemergence application assay demonstrated that 8e and 7e separately showed the best herbicidal activity at 750 g a.i./ha and lower doses (187.5 g, 375g a.i./ha) without no significant toxicity to maize and wheat. The surface plasmon resonance revealed strong binding affinity between 7e and Synechococcus PDS (SynPDS). The HPLC analysis confirmed that 8e at 750 g a.i./ha caused significant phytoene accumulation in Arabidopsis seedlings. This work demonstrates the efficacy of structure-guided optimization through scaffold hopping and linker modification to design potent PDS inhibitors with enhanced bioactivity and crop safety.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oxidorreductasas / Zea mays / Inhibidores Enzimáticos / Herbicidas Idioma: En Revista: J Agric Food Chem Año: 2024 Tipo del documento: Article Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oxidorreductasas / Zea mays / Inhibidores Enzimáticos / Herbicidas Idioma: En Revista: J Agric Food Chem Año: 2024 Tipo del documento: Article Pais de publicación: Estados Unidos