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

Environ Sci Pollut Res Int. 2019 May;26(14):13833-13838. doi: 10.1007/s11356-018-3539-0. Epub 2018 Oct 30.

Abstract

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.

Keywords: 1,1-Double phenyl acetone; 1,3-Indandione; Anticoagulant rodenticide; Feeding coefficient; Fluorouracil chloride; LD50; Phenylacetone.

MeSH terms

  • Animals
  • Anticoagulants / chemical synthesis*
  • Anticoagulants / chemistry
  • Anticoagulants / pharmacology
  • Dose-Response Relationship, Drug
  • Female
  • Indans / chemical synthesis*
  • Indans / chemistry
  • Indans / pharmacology
  • Lethal Dose 50
  • Magnetic Resonance Spectroscopy
  • Male
  • Rats
  • Rodenticides / chemical synthesis*
  • Rodenticides / chemistry
  • Rodenticides / pharmacology

Substances

  • 1,2-indanedione
  • Anticoagulants
  • Indans
  • Rodenticides