Design and Synthesis of Novel Insecticides Based on the Serotonergic Ligand 1-(4-Aminophenyl)ethyl-4- 3-(trifluoromethyl)phenylpiperazine (PAPP)

Mingyi Cai; Zhong Li; Feng Fan

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Design and Synthesis of Novel Insecticides Based on the Serotonergic Ligand 1-(4-Aminophenyl)ethyl-4- 3-(trifluoromethyl)phenylpiperazine (PAPP)

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摘要

1-(4-Aminophenyl)ethyl-4-3-(trifluoromethyl)phenylpiperazine (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-ylpiperazine derivatives were designed, synthesized, and evaluated for biological activities against the armyworm Pseudaletla 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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来源
《Journal of Agricultural and Food Chemistry》 |2010年第5期|2624-2629|共6页
作者
Mingyi Cai; Zhong Li; Feng Fan;
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作者单位

Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, P.O. Box 544, 130 Meilong Road, Shanghai 200237, People's Republic of China;

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原文格式 PDF
正文语种英语
中图分类营养卫生、食品卫生;
关键词
PAPP; 1-arylrnethyl-4-(trifluoromethyl)pyrldln-2-ylplperazlne; larvicidal activity; growth lnhibiting activity; QSAR;

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Design and Synthesis of Novel Insecticides Based on the Serotonergic Ligand 1-(4-Aminophenyl)ethyl-4- 3-(trifluoromethyl)phenylpiperazine (PAPP)

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