Abstract: Diamide insecticides with high efficacy against pests and good environmental safety are broadly applied in crop protection. They act at a poorly-defined site in the very complex ryanodine (Ry) receptor (RyR) potentially accessible to a fluorescent probe. Two N-propynyl analogs of the major anthranilic diamide insecticides chlorantraniliprole (Chlo) and cyantraniliprole (Cyan) were accordingly synthesized and converted into two fluorescent ligands by click reaction coupling with 3-azido-7-hydroxy-2H-chromen-2-one. The new diamide analogs and fluorescent ligands were shown to be nearly as potent as Chlo and Cyan in inhibition of [3H]Chlo binding and stimulation of [3H]Ry binding in house fly thoracic muscle RyR. Although the newly synthesized compounds had only moderate activity in insect larvicidal activity assays, their high in vitro potency in a validated insect RyR binding assay encourages further development of fluorescent probes for insect RyRs.
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Wang, Y.; Guo, L.; Qi, S.; Zhang, H.; Liu, K.; Liu, R.; Liang, P.; Casida, J.E.; Liu, S. Fluorescent Probes for Insect Ryanodine Receptors: Candidate Anthranilic Diamides. Molecules 2014, 19, 4105-4114.
Wang Y, Guo L, Qi S, Zhang H, Liu K, Liu R, Liang P, Casida JE, Liu S. Fluorescent Probes for Insect Ryanodine Receptors: Candidate Anthranilic Diamides. Molecules. 2014; 19(4):4105-4114.
Wang, Yi; Guo, Lei; Qi, Suzhen; Zhang, Hao; Liu, Kechang; Liu, Ruiquan; Liang, Pei; Casida, John E.; Liu, Shangzhong. 2014. "Fluorescent Probes for Insect Ryanodine Receptors: Candidate Anthranilic Diamides." Molecules 19, no. 4: 4105-4114.