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Updated: Jan 18, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Design, Synthesis, and Herbicidal Activity of Pyridinyl-benzothiazolone Heterocyclic Derivatives
Qianhong Liu1, Luyao Chen1, Jinjin Wang1
1College of Plant Protection, Northwest A&F University, Yangling, Shaanxi 712100, China.
Abstract:
Protoporphyrinogen oxidase (PPO, EC 1.3.3.4), as a key enzyme in chlorophyll biosynthesis, plays an important role in the development of novel herbicides. In this study, the 3-(pyridin-2-yl)benzothiazol-2-one scaffolds were integrated with uracil-based pharmacophores through hybridization strategies to develop innovative molecules with the dual advantages of enhancing herbicidal activity and improving crop safety. Starting from substituted anilines, a total of 25 benzothiazol-2(3H)-one derivatives were synthesized via a multistep synthetic protocol, and their structures were characterized by 1H and 13C NMR and single-crystal X-ray diffraction analysis (for B-04). Pot experiments revealed that B-04 exhibits excellent post-emergence herbicidal activity against broadleaf weeds. Notably, it demonstrates potent pre-emergence activity against both dicotyledonous and monocotyledonous weeds, showing efficacy comparable to that of flumioxazin. Furthermore, B-04 exhibited favorable crop safety as a selective pre-emergence herbicide in soybean, peanut, and cotton cultivation systems. This study developed a novel N-phenyl heterocyclic herbicide featuring a 3-(pyridin-2-yl)benzothiazol-2-one scaffold.
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