500011-92-7Relevant articles and documents
Design, synthesis, insecticidal activities, and molecular docking of novel pyridylpyrazolo carboxylate derivatives
Peng, Hongxiang,Xu, Hanhong,Yang, Shuai,Zhao, Chen,Zhu, Jinyi
, (2022/03/31)
Based on our previous work, using the strategies of “scaffold hopping” and “intermediate derivatization method” (IDM), a total of 44 novel pyridylpyrazolo carboxylate derivatives were designed and synthesized. The structures of these compounds were identified by 1H NMR and 13C NMR, and the insecticidal activities of the target compounds against Plutella xylostella and Spodoptera frugiperda were tested. Compound G35 showed the best insecticidal activities against P. xylostella (LC50?=?33.65 mg/L) and S. frugiperda (mortality rate?=?61.21% at 100 mg/L). Preliminary structure–activity relationship analysis showed that the introduction of amino group and acetamide on the benzene ring helped to improve the insecticidal activity of the scaffold. Molecular docking model between compounds G34 or G35 and Ryanodine receptors (RyRs) of P. xylostella showed that RyRs may be a potential target of this series compounds and explained the difference in insecticidal activities. These findings provided guidance for further optimization of the pyridylpyrazolo carboxylate scaffold as potential insecticide.
PROCESS FOR THE PREPARATION OF CARBOXYLIC ACID DERIVATIVES OF 3-BROMO-4,5-DIHYDRO-1H-PYRAZOLES
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Page/Page column 10-13, (2021/02/26)
Disclosed a method for preparing compound of Formula (I) and (II) wherein R1, R2, R3, X and n are as defined in the disclosure.
Design, synthesis, and insecticidal activities of novel diamide derivatives with alpha-amino acid subunits
Chen, Rui-Jia,Wang, Jun-Jie,Han, Li,Gu, Yu-Cheng,Xu, Zhi-Ping,Cheng, Jia-Gao,Shao, Xu-Sheng,Xu, Xiao-Yong,Li, Zhong
, p. 1429 - 1436 (2021/05/06)
A series of diamide derivatives containing α-amino acids were designed and synthesized. These compounds were evaluated for their insecticidal activities against Plutella xylostella, Mythimna separate, Myzus persicae, and Tetranychus cinnabarinus. Most of the title compounds containing an l-phenylglycine skeleton were endowed with good activities at the concentration of 500 mg·L?1. Compounds (R)-A6 showed a potential value for further optimization as an insecticidal lead with the LC50 value of 86.8 mg·L?1.