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

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

2019

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.

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