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- Title
Computational design of novel inhibitors to overcome weed resistance associated with acetohydroxyacid synthase ( AHAS) P197L mutant.
- Authors
Qu, Ren‐Yu; Yang, Jing‐Fang; Liu, Yu‐Chao; Chen, Qiong; Hao, Ge‐Fei; Niu, Cong‐Wei; Xi, Zhen; Yang, Guang‐Fu
- Abstract
BACKGOUND Acetohydroxyacid synthase ( AHAS; EC 2.2.1.6) is the first common enzyme in the biosynthetic pathway leading to the branched-chain amino acids in plants and a wide range of microorganisms. With the long-term and wide application of AHAS inhibitors, weed resistance is becoming a global problem, which leads to an urgent demand for novel inhibitors to antagonize both wild-type and resistant AHAS. RESULTS Pyrimidinyl salicylic acid derivatives, as one of the main classes of commercial AHAS herbicides, show potential anti-resistant bioactivity to wild-type and P197L mutant. In current work, a series of novel 2-benzoyloxy-6-pyrimidinyl salicylic acid derivatives were designed through fragment-based drug discovery. Fortunately, the newly synthesized compounds showed good inhibitory activity against both wild-type and P197L mutant. Some compounds not only had a lower resistance factor value but also showed excellent inhibitory activity against wild-type AHAS and P197L mutant. Furthermore, greenhouse experiments showed compound 11m displayed almost 100% inhibition against both wild-type and high-resistant Descurainia sophia at a dosage of 150 g a.i. ha−1. CONCLUSION The present work indicated that the 2-benzoyloxy-6-pyrimidinyl salicylic acid motif was well worth further optimization. Also, compound 11m could be used as a potential anti-resistant AHAS herbicide, which requires further research. © 2016 Society of Chemical Industry
- Subjects
HERBICIDE resistance; WEED control; PLANT enzymes; ACID derivatives; AMINO acid content of plants
- Publication
Pest Management Science, 2017, Vol 73, Issue 7, p1373
- ISSN
1526-498X
- Publication type
Article
- DOI
10.1002/ps.4460