Design, synthesis, and herbicidal activity of pyrazole benzophenone derivatives

doi:10.1039/C7RA09858H

Paper

Design, synthesis, and herbicidal activity of pyrazole benzophenone derivatives

Published Oct 2, 2017 · Ying Fu, Meng-Xia Wang, Dong Zhang

RSC Advances

Q1 SJR score

20

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0

Influential Citations

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Abstract

4-Hydroxyphenylpyruvate dioxygenase is one of the most promising targets for herbicide discovery. A series of 1-acyl-3-phenyl-pyrazol benzophenones were designed and synthesized using 1,3-diphenylpropane-1,3-dione and dimethylformamide dimethylacetal as the starting materials. All of the compounds were characterized by IR, 1H NMR, 13C NMR, and HRMS. The configuration of 5f was determined by X-ray crystallography. The bioassay studies indicated that most of these derivatives exhibited herbicidal activity at least to a certain degree, in which compounds 5n and 5o displayed good herbicidal activity at a dosage of 0.05 mmol m−2, which were more potent than pyrazoxyfen against barnyard grass. In addition, compound 5o was also proved to be safer for maize than pyrazoxyfen. The binding free energy of compound 5o with HPPD was relatively low, and that agreed with the results of bioassay activity research. Therefore, compound 5o might be the lead compound for designing new HPPD inhibitors.

Study Snapshot

Compound 5o shows potential as a lead compound for designing new HPPD inhibitors, with more potent herbicidal activity against barnyard grass and a safer maize toxicity than pyrazoxyfen.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Design, synthesis, and herbicidal activity of pyrazole benzophenone derivatives

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