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Discovery of FM-2665 as a Potent Arylpyrazole Insecticidal and Acaricidal Candidate: Rational Design via Pyridine
Xiaowen Du1, Dongdong Liu1, Qingjie Bi1
1National-Local Joint Engineering Laboratory for Development of Boron and Magnesium Resources and Fine Chemical Technology, Liaoning Province Key Laboratory of Green Functional Molecular Design and Development, Shenyang Key Laboratory of Targeted Pesticides, Institute of Functional Molecules, Shenyang University of Chemical Technology, Shenyang110142, China.
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Sixteen novel arylpyrazole derivatives were designed using tigolaner as a scaffold reference and synthesized to examine the effects of pyridine bioisosterism and terminal alkyl modification. Among the synthesized compounds, FM-2665 (A14) showed the highest overall activity against Plutella xylostella, Tetranychus cinnabarinu, and Myzus persicae, with LC50 values of 0.127, 0.604, and 0.496 mg/L, respectively. On the basis of the LC50 values, FM-2665 was 6.68-fold more potent than tigolaner against P. xylostella. Molecular docking and DFT calculations suggested that additional predicted contacts involving Gln96 and Val126, together with a narrower HOMO-LUMO gap, may contribute to the observed structure-activity relationship. These calculations do not establish receptor affinity, and direct functional validation of GABAR antagonism remains necessary. FM-2665 therefore represents a promising lead for further optimization and safety evaluation.
