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Insect pharyngeal voxin antagonist and use thereof

A pharyngeal-promoting side voxel and antagonist technology, applied in the field of pesticides, can solve the problems of affecting the environment, pesticide residues, etc., and achieve the effects of regulating absorption and good application prospects

Inactive Publication Date: 2017-07-18
SHANGHAI INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Aiming at the above-mentioned technical problems in the prior art, the present invention provides an antagonist of insect pharyngeal voxel and its use, which solves the problem of the existing Pesticides in the technology will have residues, technical issues affecting the environment

Method used

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  • Insect pharyngeal voxin antagonist and use thereof
  • Insect pharyngeal voxin antagonist and use thereof
  • Insect pharyngeal voxin antagonist and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The preparation of embodiment 1 compound I1 (L-alanyl-L-arginyl-glycyl-L-phenylalaninamide)

[0034]

[0035] (1) Resin activation: Weigh 200mg Rink Amide-AM resin, wash 4 times with dichloromethane, add 15ml dichloromethane to swell and activate for 3 hours, wash 4 times with N,N-dimethylformamide, add 20% piperidine Cut with N,N-dimethylformamide solution for 20min, wash 4 times with 5ml N,N-dimethylformamide, wash 4 times with 5ml dichloromethane, and detect with Kaiser's reagent.

[0036](2) Phenylalanine: N,N-dimethylformamide washed 3 times, added 116mg phenylalanine protected by fluorene methoxycarbonyl, 114mg O-benzotriazole-tetramethylureahexa Fluorophosphate (HBTU), 41mg 1-hydroxybenzotriazole (HOBt), 105ul N,N-diisopropylethylamine (DIEA), dissolved in 15ml N,N-dimethylformamide, stirred at room temperature for 2h, 5ml Wash 4 times with N,N-dimethylformamide, add 20% piperidine in N,N-dimethylformamide, cut for 20min, wash 4 times with 5ml N,N-dimethylfor...

Embodiment 2

[0043] The preparation of embodiment 2 compound I5 (L-alanyl-L-arginyl-2,2-difluoroglycyl-L-phenylalaninamide)

[0044]

[0045] (1) Resin activation: Weigh 200mg Rink Amide-AM resin, wash 4 times with dichloromethane, add 15ml dichloromethane to swell and activate for 3h, wash 4 times with N,N-dimethylformamide, add 20% piperidine The N,N-dimethylformamide solution was cut for 20min, washed 4 times with 5ml N,N-dimethylformamide, washed 4 times with 5ml dichloromethane, and detected by Kaiser's reagent.

[0046] (2) Phenylalanine: N,N-dimethylformamide washed 3 times, added 116mg phenylalanine protected by fluorene methoxycarbonyl, 114mg O-benzotriazole-tetramethylureahexa Fluorophosphate (HBTU), 41mg 1-hydroxybenzotriazole (HOBt), 105ul N,N-diisopropylethylamine (DIEA), dissolved in 15ml N,N-dimethylformamide, stirred at room temperature for 2h , washed 4 times with 5ml N,N-dimethylformamide, added 20% piperidine in N,N-dimethylformamide solution for cutting for 20min, w...

Embodiment 3

[0053] The preparation of embodiment 3 compound I9 (L-alanyl-L-arginyl-glycyl-L-4-fluorophenylalaninamide)

[0054]

[0055] (1) Resin activation: Weigh 200mg Rink Amide-AM resin, wash 4 times with dichloromethane, add 15ml dichloromethane to swell and activate for 3h, wash 4 times with N,N-dimethylformamide, add 20% piperidine The N,N-dimethylformamide solution was cut for 20min, washed 4 times with 5ml N,N-dimethylformamide, washed 4 times with 5ml dichloromethane, and detected by Kaiser's reagent.

[0056] (2) Fluorophenylalanine: N,N-dimethylformamide washed 3 times, added 121mg Fmoc-Phe(4-F)-OH, 114mg HBTU, 41mg HOBt, 105ul DIEA, dissolved in 15ml N ,N-dimethylformamide, stirred at room temperature for 2h, washed 4 times with 5ml N,N-dimethylformamide, added 20% piperidine in N,N-dimethylformamide solution for cutting for 20min, 5ml N,N - Wash 4 times with dimethylformamide, 4 times with 5 ml of dichloromethane, and detect with Kaiser's reagent.

[0057] (3) Glycine:...

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Abstract

The invention belongs to the field of pesticides and provides an insect pharyngeal side voxel antagonist, the structure of which is shown in formula I: The present invention also provides the application of the above-mentioned insect pharyngeal side voxel antagonist in controlling pests. The compound of the present invention has excellent antagonistic effect on pharyngophorin, and its inhibitory concentration reaches nanomol per liter; and its structure is relatively simple compared with pharyngotropin and other insect neuropeptide hormones, and is easy to apply.

Description

technical field [0001] The invention belongs to the field of pesticides, and in particular relates to an insecticide, in particular to an antagonist of insect pharyngeal voxin and its use. Background technique [0002] As a plant protection tool that can effectively control crop diseases, insects, and weeds, pesticides can save 30%-40% of the world's total crop output loss and economic losses of about 300 billion U.S. dollars every year. Traditional insecticides have made outstanding contributions to the efficient and rapid control of pests, the protection of crop harvests and human health. But at the same time, due to people's irrational use of pesticides, coupled with the inherent shortcomings of some pesticides, a series of problems have been caused: such as residues, pollution to the environment, negative impact on ecology, and harm to humans, animals, natural enemies and Damage to non-target organisms, etc. With the increasing awareness of human environmental protecti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K5/103C07K5/09A01N47/44A01P7/04
Inventor 开振鹏李媛媚王志杨新玲邓希乐
Owner SHANGHAI INST OF TECH
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