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The research of synthesis and bioactivity of the novel indanedione anticoagulant rodenticides

Chen, Feng, Zhang, Tong, Qu, Chuang, Wang, Jinming, Su, Hua, Shi, Ruofan, Zhu, Xingyu
Environmental science and pollution research international 2019 v.26 no.14 pp. 13833-13838
acute toxicity, anticoagulants, coumarin, death, fluorides, fluorine, lethal dose 50, medicine, nuclear magnetic resonance spectroscopy, palatability, rats, rodenticides
Three new anticoagulant rodenticides R₁, R₂, and R₃ were designed. The containing fluorine acute toxicity groups was added to 1,3-indandione derivative. Analysis method of synthesized anticoagulant rodenticides were IR, ¹H NMR. Acute bioactivity of the new rodenticides was evaluated, including the coefficient of absorb food and median lethal dose (LD₅₀). Average coefficient of absorbed food for R₁ was 0.54 and LD₅₀ of R₁ was 2.15 mg/kg. Average coefficient of absorbed food for R₂ was 0.59 and the acute oral LD₅₀ of R₂ was 2.65 mg/kg. Average feeding coefficient of R₃ was 0.68 and the acute oral LD₅₀ of R₃ was 3.12 mg/kg. Experiments showed that rat’s death peak was at about 72 h and rodenticides had good characteristics of acute medicine. The LD₅₀ of three new fluoride anticoagulant rodenticides showed that they had good palatability for big white rats, and they had a strong poison effect on rodent. The result of all experiments proved that the synthesis of 1,3-indan diketone used as parent compound of new anticoagulant rodenticides could replace the current 4-hydroxyl coumarin as parent compound of the second-generation anticoagulant rodenticides. 1,3-Indan diketone would be widely used as parent compound of anticoagulant rodenticides.