Synthesis, nematocidal activity and SAR study of novel difluoromethylpyrazole carboxamide derivatives containing flexible alkyl chain moieties

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• 作者：Xing-Hai Liu^a ; ^{xhliu@zjut.edu.cn} ; Wen Zhao^a ; ^b ; Zhong-Hua Shen^a ; Jia-Hua Xing^b ; Tian-Ming Xu^b ; Wei-Li Peng^b ; ^{pengweili@sinochem.com}
• 关键词：Difluoromethylpyrazole carboxamide ; Flexible chain ; Nematicidal activity ; Docking
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：881-889
• 全文大小：857 K
• 卷排序：125

文摘

The novel difluoromethylpyrazole derivatives containing flexible alkyl chain moieties were designed and synthesized. Compound 6-9 and 6-23 possessed most good nematocidal activity against M. incognita with low toxicity. Compound 6-9 also exhibited low toxicity against rat and no eye or skin sensitization against rabbit. Molecular docking study suggested that the flexible NHCOO group of compound 6-9 inhibited the acetylcholine receptor (AChR).