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

In this study, a series of novel mesoionic pyrido[1,2-a]pyrimidinone compounds containing a natural skeleton indole were designed and synthesized, and the insecticidal activities of the target compounds were tested. The results showed that the target compounds had good to excellent insecticidal activities against white-backed planthoppers (Sogatella furcifera) and bean aphids (Aphis craccivora). Among them, compound 7 showed outstanding insecticidal activities against both S. furcifera and A. craccivora, with LC₅₀ values of 0.86 and 0.85 μg/mL, respectively. The insecticidal activity against bean aphids (A. craccivora) was superior to that of triflumezopyrim (LC₅₀ = 3.67 μg/mL). Proteomics and quantitative real-time polymerase chain reaction (qRT-PCR) results revealed that compound 7 may interact with α1 and α7 nAChR subunits of S. furcifera. The results of enzyme activities indicated that compound 7 was an inhibitor of AChE in S. furcifera. This study provides new ideas for the discovery of new mesoionic pyrido[1,2-a]pyrimidinone insecticides.