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Design and synthesis of novel insecticides based on the serotonergic ligand 1-[(4-aminophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl]piperazine (PAPP)
- Source :
- Journal of agricultural and food chemistry. 58(5)
- Publication Year :
- 2009
-
Abstract
- 1-[(4-Aminophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl]piperazine (PAPP) is a 5-HT(1A) agonist and was reported to display high affinity for serotonin (5-HT) receptor from the parasitic nematode Haemonchus contortus . The present investigation explored the possibility of using PAPP as a lead compound of new insecticides with novel mode of action. On the basis of the PAPP scaffold, a series of 1-arylmethyl-4-[(trifluoromethyl)pyridin-2-yl]piperazine derivatives were designed, synthesized, and evaluated for biological activities against the armyworm Pseudaletia separata (Walker). Bioassays showed that most of the target compounds displayed certain growth-inhibiting activities or larvicidal activities against armyworm. The quantitative structure-activity relationship (QSAR) for growth-inhibiting activities was also analyzed and established.
- Subjects :
- Agonist
Quantitative structure–activity relationship
Insecticides
Spectrometry, Mass, Electrospray Ionization
Trifluoromethyl
Magnetic Resonance Spectroscopy
Spectrophotometry, Infrared
medicine.drug_class
Ligand
Stereochemistry
Quantitative Structure-Activity Relationship
General Chemistry
Nuclear magnetic resonance spectroscopy
Moths
Ligands
Piperazines
chemistry.chemical_compound
Piperazine
chemistry
Receptors, Serotonin
medicine
Animals
General Agricultural and Biological Sciences
Mode of action
Lead compound
Subjects
Details
- ISSN :
- 15205118
- Volume :
- 58
- Issue :
- 5
- Database :
- OpenAIRE
- Journal :
- Journal of agricultural and food chemistry
- Accession number :
- edsair.doi.dedup.....a70a078594eda1d16a86380807f07749