59229-45-7Relevant articles and documents
The application of "plug-in molecules" method in novel strobilurin fungicides screening
Fu, Bin,Li, Jia-Qi,Liu, Xuelian,Qin, Zhaohai,Xiao, Yumei,Yang, Dongyan,Yin, Fahong
, p. 42804 - 42809 (2020)
Based on the "plug-in molecular"method, a series of novel strobilurin derivatives with aryloxypyridinyl-1-ethanone oxime side chains were designed, synthesized, and screened. The biological activity experiment showed that they had an excellent fungicidal effect on plant pathogens, especially Sclerotinia sclerotiorum. Compounds 5-01 and 5-09 had significant fungicidal activity and broad fungicidal spectrum. The structure-Activity relationship indicates that the cis configuration, increasing the number of pharmacophores, substitution of the 2 position of the pyridine ring, and the introduction of chlorine atom on the benzene ring were not conducive to the fungicidal activity of such compounds. The model of 3D-QSAR indicated the introduction of large electropositive groups at the 4 position of the benzene ring and the introduction of small electronegative groups at the 2 position of the benzene ring were beneficial to the fungicidal activity, and compounds 6 were designed. Compared with azoxystrobin, compound 6-02 had a more effective fungicidal effect against Sclerotinia sclerotiorum (Lib.) de Bary. Cytotoxicity test and transmission electron microscopy showed that the modification of strobilurins fungicide by the "plug-in molecular"method would not affect its toxicity and mechanism. The "plug-in molecular"method is an efficient method for screening highly active compounds, which has important guiding significance for creating new pesticide molecules. This journal is
Pymetrozine derivative and its preparation method and application of parasite killing
-
Paragraph 0037; 0038; 0039; 0040, (2018/07/07)
The invention relates to a pymetrozine derivative (I) and a preparing method and insecticidal application thereof. According to a formula of the pymetrozine derivative (I), groups' meanings are shown in an instruction. The pymetrozine derivative (I) has excellent activity of killing aphids and insecticidal activity of killing mosquito larvae, cotton bollworms, European corn borers and armyworms.
Design, Synthesis, and Structure-Activity Relationship of New Pyrimidinamine Derivatives Containing an Aryloxy Pyridine Moiety
Guan, Aiying,Liu, Changling,Chen, Wei,Yang, Fan,Xie, Yong,Zhang, Jinbo,Li, Zhinian,Wang, Mingan
, p. 1272 - 1280 (2017/02/23)
The pyrimidinamine diflumetorim is an ideal template for the discovery of agrochemical lead compounds due to its unique mode of action, novel chemical structure, and lack of reported resistance. To develop a new pyrimidinamine fungicide effective against cucumber downy mildew (CDM), a series of new pyrimidinamine derivatives containing an aryloxy pyridine moiety were designed and synthesized by employing the recently reported intermediate derivatization method (IDM). The structures of all compounds were identified by 1H NMR, elemental analyses, HRMS, and X-ray diffraction. Bioassays demonstrated that some of the title compounds exhibited excellent fungicidal activities against CDM. Compound 9 gave the best activity (EC50 = 0.19 mg/L), which is significantly better than the commercial fungicides diflumetorim, flumorph, and cyazofamid. The relationship between structure and fungicidal activity of the synthesized pyrimidinamines was explored. The study showed that compound 9 is a promising fungicide candidate for further development.
