59229-45-7Relevant academic research and scientific papers
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
Design, synthesis, and biological activity of sulfoximine derivatives
Fu, Bin,Li, Jiaqi,Liu, Yanfei,Qin, Zhaohai,Wang, Mian,Wu, Yanhua,Xiao, Yumei,Xu, Yanjun
, (2021/12/30)
In order to discover new pesticides with novel modes of action and further study the sulfoximine scaffolds, 30 novel sulfoximine derivatives were designed, synthesized, and evaluated for their insecticidal and antifungal activities. The preliminary bioassay results showed that the insecticidal activity of target compounds was weak, only I-12 displayed 80.39% larvicidal activity against Nilaparvata lugen, slightly lower than sulfoxaflor (97.87%) at 100 μg/ml. However, most of the compounds also displayed fair to good fungicidal activities against eight representative phytopathogenic fungi, and I-5 showed slightly lower fungicidal activity against Sclerotinia scleotiorum than the control drug difenoconazole (2.26 μg/ml) with an EC50 of 8.75 μg/ml. The structure–activity relationship showed that the compound exhibited better antifungal activity when the R was 2.4-disubstituted phenyl. Our studies suggested that sulfoximine scaffolds may also have potential plant-fungal activity. This is the first report on the use of sulfoximide scaffolds as fungicides.
Pymetrozine derivative and its preparation method and application of parasite killing
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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.
BTK INHIBITOR
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, (2017/11/16)
Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).
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.
Additive effects on the improvement of insecticidal activity: Design, synthesis, and insecticidal activity of novel pymetrozine derivatives
Yang, Yan,Liu, Yuxiu,Song, Hongjian,Li, Yongqiang,Wang, Qingmin
, p. 391 - 402 (2016/01/25)
A series of new pymetrozine analogues containing both methyl on the imine carbon and phenoxy group at the pyridine ring were designed and synthesized. Their insecticidal activities against bean aphid (Aphis craccivora), mosquito larvae (Culex pipiens pallens), cotton bollworm (Helicoverpa armigera), corn borer (Ostrinia nubilalis) and oriental armyworm (Mythimna separata) were evaluated. The results of bioassays indicated that most of the target compounds showed good insecticidal activity against bean aphid; especially, IIIf (80%) and IIIl (80%) exhibited higher aphicidal activity than pymetrozine (30%) at 5 mg/kg, and the two compounds still showed 20% and 30% mortality at 2.5 mg/kg, respectively, whereas pymetrozine displayed no activity at the same concentration. These compounds exhibited a completely different structure-activity relationship to that of known pymetrozine derivatives, in which it is thought introducing alkyl group on the imine carbon could be detrimental to the activities. Our new result suggested that the methyl on the imine carbon and phenoxy group at the pyridine ring of phenoxy group may play additive effects on the improvement of aphicidal activity. Besides this, compound IIIs, containing an allyl at the para position of phenoxy group, exhibited excellent insecticidal activity against mosquito larvae, lepidoptera pests cotton bollworm, corn borer and oriental armyworm.
Cycloauration of substituted 2-phenoxypyridine derivatives and X-ray crystal structure of gold, dichloro[2-[[5-[(cyclopentylamino) carbonyl]-2-pyridinyl-κN]oxy]phenyl-κC]-, (SP-4-3)-
Zhu, Yongbao,Cameron, Beth R.,Skerlj, Renato T.
, p. 57 - 72 (2007/10/03)
Direct cycloauration of 2-phenoxypyridines with different substituents at the 5-position of the pyridine ring was carried out in an CH3CN/H2O medium, leading to isolation of cycloaurated compounds AuCl2(L) (HL = substitute
