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To obtain new elicitors that could induce plant defense against pests, a series of furan carbonylhydrazones were synthesized. Phenotypic high-throughput screening of β-glucuronidase (GUS) activity was used to identify elicitors with strong activity. Integrated bioassays were conducted to acquire chemical elicitors that induce resistance in rice to the brown planthopper Nilaparvata lugens and they are not direct toxic to the pest. Our results demonstrate that these compounds have the potential to serve as new kinds of environment-friendly plant protection agents in rice.

Herein, we report the first access of β-elemene derivatives through the SeO 2 -mediated oxidation reaction. Several new compounds were isolated through such a one-step reaction, and their structures were elucidated using various 2D-NMR techniques. This method provides easy access to multiple oxidative β-elemene derivatives in one single step and represents the first modifications on cyclohexyl ring of β-elemene. It is expected to open up the opportunity for future derivatization on cyclohexyl ring of β-elemene. The new compounds obtained above showed better anti-proliferation activities than β-elemene itself on several cancer cell lines. Among them, compound 17 shows the best activity in antiproliferation assays of A549 and U-87MG cell lines.

Natural products are a major source of biological molecules. The 3‐methylfuran scaffold is found in a variety of plant secondary metabolite chemical elicitors that confer host‐plant resistance against insect pests. Herein, the diversity‐oriented synthesis of a natural‐product‐like library is reported, in which the 3‐methylfuran core is fused in an angular attachment to six common natural product scaffolds—coumarin, chalcone, flavone, flavonol, isoflavone and isoquinolinone. The structural diversity of this library is assessed computationally using cheminformatic analysis. Phenotypic high‐throughput screening of β‐glucuronidase activity uncovers several hits. Further in vivo screening confirms that these hits can induce resistance in rice to nymphs of the brown planthopper Nilaparvata lugens. This work validates the combination of diversity‐oriented synthesis and high‐throughput screening of β‐glucuronidase activity as a strategy for discovering new chemical elicitors.

Herein we report a new way to identify chemical elicitors that induce resistance in rice to herbivores. Using this method, by quantifying the induction of chemicals for GUS activity in a specific screening system that we established previously, 5 candidate elicitors were selected from the 29 designed and synthesized phenoxyalkanoic acid derivatives. Bioassays confirmed that these candidate elicitors could induce plant defense and then repel feeding of white-backed planthopper Sogatella furcifera.