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Synthesis, Biological Activities, and SAR Studies of Novel 1-(2-chloro-4,5-difluorophenyl)-1H-pyrazole Derivatives.

Authors
  • Zhao, Yangyang1
  • Li, Huangong1
  • Sun, Pengwei1
  • Gao, Li1
  • Liu, Jingbo1
  • Zhou, Sha1
  • Xiong, Lixia1
  • Yang, Na1
  • Li, Yuxin1
  • Li, Zhengming1
  • 1 State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China. , (China)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Sep 05, 2020
Pages
127535–127535
Identifiers
DOI: 10.1016/j.bmcl.2020.127535
PMID: 32898692
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

In order to search for the new ryanodine receptor (RyR) regulator, a series of 35 novel fluoro-substituted compounds introduced 1-(2-chloro-4,5-difluorophenyl)-1H-pyrazole moiety containing modified pyrazole heterocycle were designed and synthesized. Then, they were tested for the insecticidal activities against Mythimna separata and Plutella xylostella in our greenhouse. After a systematic biological screening, it was found out that IVc showed 50% larvicidal activities against Mythimna separata at 0.1 mg L-1, equivalent to that of chlorantraniliprole (36%, 0.1 mg L-1). The activity of IVc against Plutella xylostella was 90% at 10-5 mg L-1, whereas the chlorantraniliprole was 70% at the same concentration. Then, insect electrophysiology experiments were conducted to study the pattern of action of IVc and IVe. It was confirmed by the experimental results that both compounds could lead to the release of calcium from the endoplasmic reticulum of neurons as classical anthranilic diamide insecticides. Copyright © 2020. Published by Elsevier Ltd.

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