| 20000410 |
Cai M, Li Z, Fan F, Huang Q, Shao X, Song G: Design and synthesis of novel insecticides based on the serotonergic ligand 1-[(4-aminophenyl) ethyl]-4-[3-(trifluoromethyl) phenyl] piperazine (PAPP). J Agric Food Chem. 2010 Mar 10;58(5):2624-9.
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. |
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