Design, Synthesis, and Insecticidal Activity of Novel Pyrido[1,2-?]pyrimidinone Mesoionic Compounds Containing an IndoleMoiety as Potential Acetylcholine Receptor Insecticides

Hu, Deyu ¹Zhang, Jian ¹Song, Runjiang ¹Song, Baoan ¹Wu, Shang ¹Cai, Di ¹Wu, Zengxue¹

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作者信息

1. Guizhou Univ
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Abstract

In this study, a series of novel mesoionic pyrido[1,2-a]pyrimidinone compounds containing a natural skeleton indolewere designed and synthesized, and the insecticidal activities of the target compounds were tested. The results showed that the targetcompounds had good to excellent insecticidal activities against white-backed planthoppers (Sogatella furcifera) and bean aphids(Aphis craccivora). Among them, compound7showed outstanding insecticidal activities against bothS. furciferaandA. craccivora,with LC50values of 0.86 and 0.85 mu g/mL, respectively. The insecticidal activity against bean aphids (A. craccivora) was superior tothat of triflumezopyrim (LC50= 3.67 mu g/mL). Proteomics and quantitative real-time polymerase chain reaction (qRT-PCR) resultsrevealed that compound7may interact with alpha 1 and alpha 7 nAChR subunits ofS. furcifera. The results of enzyme activities indicated thatcompound7was an inhibitor of AChE inS. furcifera. This study provides new ideas for the discovery of new mesoionic pyrido[1,2-a]pyrimidinone insecticides.

Key words

mesoionic/pyridopyrimidinone/indole/insecticidal activity/nicotinic acetylcholine receptors/NEONICOTINOID INSECTICIDES/TRIFLUMEZOPYRIM/DISCOVERY/RESISTANCE/ALKALOIDS

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出版年

2022

Journal of Agricultural and Food Chemistry

CCREI

ISSN：0021-8561

被引量7

参考文献量37

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