500011-88-1Relevant articles and documents
Diamides conformationally restricted with central amino acid: Design, synthesis, and biological activities
Chen, Rui-Jia,Cheng, Jia-Gao,Dong, Le-Feng,Feng, Ting-Ting,Gu, Yu-Cheng,Li, Zhong,Shao, Xu-Sheng,Wang, Gang-Ao,Wang, Jun-Jie,Xu, Xiao-Yong,Xu, Zhi-Ping,Zhou, Cong
, (2022/02/03)
Diamide insecticides, represented by chlorantraniliprole (CHL), were widely applied in the control of lepidopteran insects. In efforts to develop bioactive diamides with novel scaffolds, we design and synthesized a series of diamides containing central amino acids to conformationally simulate CHL. Bioassay results indicated that most compounds containing 1-aminocyclopropane-1-carboxylic acid exhibited excellent larvacidal potency against Mythimna separate and Plutella xylostella. After a systematic structure–activity relationship study, 1–23 was identified as a potential insecticidal candidate with LC50 values of 34.920 mg·L?1 against M. separate and 61.992 mg·L?1 on P. xylostella. Finally, molecular docking revealed the possible binding mode of 1–23 with the target protein, ryanodine receptors.
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.
N-ALKYL-N-CYANOALKYLBENZAMIDE COMPOUND AND USE THEREOF
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, (2021/01/25)
The present invention discloses an N-alkyl-N-cyanoalkylbenzamide compound of General Formula I, an intermediate of General Formula II used to prepare the compound, wherein R1 is selected from halo or C1-C3 alkyl; R2