- Study of the synthesis, antiviral bioactivity and interaction mechanisms of novel chalcone derivatives that contain the 1,1-dichloropropene moiety
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A series of novel chalcone derivatives that contain the 1,1-dichloropropene moiety was designed and synthesized. Bioactivity assays showed that most of the target compounds exhibited moderate to good antiviral activity against tobacco mosaic virus (TMV) at 500?μg/mL. Among the target compounds, compound 7h showed the highest in vivo inactivation activity against TMV with the EC50 and EC90 value of 45.6 and 327.5?μg/mL, respectively, which was similar to that of Ningnanmycin (46.9 and 329.4?μg/mL) and superior to that of Ribavirin (145.1 and 793.1?μg/mL). Meanwhile, the microscale thermophoresis and fluorescence spectroscopy experiments showed that the compound 7h had a strong interaction with the tobacco mosaic virus coat protein.
- Dong, Liang-Run,Hu, De-Yu,Wu, Zeng-Xue,Chen, Ji-Xiang,Song, Bao-An
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supporting information
p. 1566 - 1570
(2017/07/17)
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- Design, synthesis and insecticidal evaluation of aryloxy dihalopropene derivatives
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Plutella xylostella (P. xylostella) is a highly migratory, cosmopolitan species and one of the most important pest of cruciferous crops worldwide. Pyridalyl as a novel class of insecticides has good efficacy against P. xylostella. On the basis of the commercial insecticide pyridalyl, a series of new aryloxy dihalopropene derivatives were designed and synthesized by using Intermediate Derivatization Methods. Their chemical structures were confirmed by 1H NMR, high-resolution mass spectrum (HRMS), and single-crystal X-ray diffraction analysis. The insecticidal activities of the new compounds against P. xylostella were evaluated. The results of bioassays indicated that most of the compounds showed moderate to high activities at the tested concentration, especially compounds 10e and 10g displayed more than 75% insecticidal activity against P. xylostella at 6.25 mg/L, while pyridalyl showed 50% insecticidal activity at the same concentration. The field trials result of the insecticidal activities showed that compound 10e as a 10% emulsifiable concentrate (EC) was effective in the control of P. xylostella at 75-150 g a.i./ha, and the mortality of P. xylostella for treatment with compound 10e at 75 g a.i./ha was equivalent to pyridalyl at 105 g a.i./ha.
- Yang, Ji-Chun,Li, Miao,Wu, Qiao,Liu, Chang-Ling,Chang, Xiu-Hui
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p. 383 - 390
(2016/01/25)
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- Chalcone derivate with 1,1-dichloropropene and preparation method and application thereof
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The invention discloses a chalcone derivate with 1,1-dichloropropene and a preparation method and application thereof. The general structural formula of the chalcone derivate is shown in the description. R is a benzene ring, a substituted aromatic ring and a heterocyclic ring, the ortho-position, meta-position and para-position of the aromatic ring contain one or more of methyl, methoxyl, trifluoromethyl, trifluoromethoxy, nitryl and halogen atoms, halogen atoms can be fluorine, chlorine and bromine, and the heterocyclic ring is a five-membered heterocyclic ring. The chalcone derivate with the 1,1-dichloropropene can improve biological activity, is low in toxicity and environmentally friendly and can be used for pesticides used for preventing and treating the tobacco mosaic virus.
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Paragraph 0016
(2016/10/08)
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- Design, synthesis and bioactivities of novel dichloro-allyloxy-phenol-containing pyrazole oxime derivatives
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In this study, in order to find novel biologically active pyrazole oxime compounds, a number of dichloro-allyloxy-phenol-containing pyrazole oximes were designed and synthesized according to the method of active group combination. All of the target compounds were confirmed by 1H-NMR, 13C-NMR and elemental analysis. In addition, bioassays showed that all of the newly synthesized compounds had no acaricidal activity against Tetranychus cinnabarinus and low insecticidal activity against Aphis craccivora at tested concentrations. However, most of them displayed excellent insecticidal activity against Oriental armyworm at a concentration of 500 μg/mL, and some designed compounds still exhibited potent insecticidal activity against Oriental armyworm even at the dose of 20 μg/mL, especially compounds 7f, 7n and 7p had 100%, 90% and 90% inhibition rates, respectively, which were comparable to that of the control pyridalyl.
- Dai, Hong,Ye, Linyu,Zhuang, Huiyang,Dai, Baojiang,Fang, Yuan,Shi, Yujun
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p. 21870 - 21880
(2016/01/25)
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- Ether Compounds with Nitrogen-Containing 5-Member Heterocycle and Uses Thereof
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The invention relates to ether compounds with nitrogen-containing 5-member heterocycle, represented by formula (I): The groups are as defined as specification. The compounds of the present invention have broad-spectrum insecticidal activities, and they ar
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Page/Page column 21
(2011/08/04)
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- Oxime compounds, their use, and intermediates for their production
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Oxime compounds of formula (1) wherein R1, R2, and R3 are independently halogen, C1-C3 alkyl, C1-C3 halolalkyl, C1-C3 alkoxy, C1-C3 haloalkoxy, nitro, or cyano; R4 is 3,3-dihalogeno-2-propenyl; a is an integer of 0 to 2; Y is oxygen, sulfur, or NH; Z is oxygen, sulfur, or NR5wherein R5 is hydrogen, acetyl, or C1-C3 alkyl; and X is of formula (2) insecticidal/acaricidal agents containing them as active ingredients; and intermediates for their production.
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- Dihalopropene compounds, insecticidal/acaricidal agents containing same, and intermediates for their production
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The dihalopropene compounds of the general formula ?I! have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.
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- Dihalopropene compounds, insecticides containing them as active ingredients, and intermediates for their production
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The present invention provides dihalopropene compounds of the general formula: STR1 wherein R1 is C1 -C10 alkyl or the like; L is C(=O)NH or the like; R2, R3 and R4 are independently haloge
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