Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

A kind of pentapeptide analogue of insect antipharyngeal side voxel and its application

A carrier and drug technology, applied in applications, peptides, pesticides, etc., can solve the problems of complex structure, unsuitability for development, high synthesis cost, and achieve the effect of simple synthesis

Active Publication Date: 2021-11-02
CHINA AGRI UNIV
View PDF8 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still the following disadvantages: the structure of the compound is complex (simulating the active peptide above pentapeptide), some structures are even more complex than natural peptides, and the synthesis cost is high, so it is not suitable for development as a new pesticide

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of pentapeptide analogue of insect antipharyngeal side voxel and its application
  • A kind of pentapeptide analogue of insect antipharyngeal side voxel and its application
  • A kind of pentapeptide analogue of insect antipharyngeal side voxel and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] The compound of formula A of the present invention is prepared according to the method of polypeptide solid-phase synthesis.

[0044] Taking compound A1 as an example, its preparation method is as follows:

[0045] (1) Resin activation: Weigh 440mg Rink Amide-AM resin, activate it with 5mL DCM for 3h, add 20% piperidine DMF solution to cut for 20min, wash with DMF and DCM for 3 times, monitor the reaction with Kaiser’s reagent.

[0046] (2) Connect to Leu: add Fmoc-Leu-OH (3 times equivalent), HBTU (3 times equivalent), HOBt (3 times equivalent), DIEA (6 times equivalent), dissolve in 5mL DMF, stir at room temperature for 2h, remove The reaction solution was washed three times with DMF and DCM, and the reaction was monitored by Kaiser's reagent. Then add 20% piperidine DMF solution to cut for 20min, and wash 3 times with DMF.

[0047] (3) Gly connection: add Fmoc-Gly-OH (3 times equivalent), HBTU (3 times equivalent), HOBt (3 times equivalent), DIEA (6 times equivalen...

Embodiment 2

[0058] Example 2 In vitro inhibitory activity of the compounds of the present invention on the biosynthesis of juvenile hormone in the Pacific cockroach

[0059] The present invention adopts the GC-MS / MS bioassay method of Kai Zhenpeng et al. (reference: Kai, Z.P.; Yin, Y.; Zhang, Z.R.; Huang, J.; Tobe, S.S.; Chen, S.S.J. , 1538, 67). The newly emerged female adults were collected, and after the 7th day, they were dissected to obtain the pharyngeal body. The target compound was made into a 10mmol / L mother solution, which was successively diluted into 1mmol / L, 0.1mmol / L, 0.01mmol / L, 0.001mmol / L and 0.0001mmol / L assay solutions. Then use a 1-10uL pipette gun to take 10uL of different concentrations of the measurement solution and add it to a 1.5mL centrifuge tube containing 990uL M199 medium. After mixing thoroughly, the obtained concentrations are 0.01mmol / L, 0.001 mmol / L, 0.0001 mmol / L, 0.00001 mmol / L, and 0.000001 mmol / L. Measure 100uL of the prepared medicinal solution an...

Embodiment 3

[0061] Embodiment 3 The biological activity of some compounds of the present invention to Plutella xylostella under the condition of 200mg / L

[0062] The application of the pentapeptide analogue of a class of insect depressor pharyngeal voxin as described in any one of claims 1-3 in the prevention and treatment of diamondback moth. The screening method for insecticidal activity against Plutella xylostella is as follows: use the leaf soaking method to conduct preliminary screening of the activity of samples at a concentration of 200mg / L; select standard test insects that are continuously reared in the room and have consistent physiological states. The original drug is dissolved with a small amount of DMF, and then diluted with 0.05% TritonX-100 aqueous solution. Each concentration was repeated 4 times, with 30 test insects for each repetition, and a blank control was set; the cabbage leaves that had grown straight were selected, immersed in 200mg / L liquid medicine for 5s, dried...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention belongs to the technical field of insecticides, and in particular relates to a pentapeptide analog of insect pharyngeal-suppressing side voxel and its application. The application proposes a compound represented by formula A, which has the following structure: wherein: R 1 R 2 from-CH 2 COOH or -CH 2 CONH 2 ; 3 from 4‑NO 2 , 4‑F, 4‑Cl, 4‑Br, 4‑CF 3 , 4-OH, 4-CH 3 , 4‑OCH 3 , 4‑OCH 2 CH 3 , 3,4,5-trimethoxy, 4-N,N-dimethyl or 4-phenyl. The compound of the invention is safe and efficient, easy to synthesize, and has potential development and application prospects.

Description

technical field [0001] The invention belongs to the technical field of insecticides, and in particular relates to a pentapeptide analog of insect pharyngeal side voxel and its application. Background technique [0002] Traditional pesticides have made outstanding contributions to pest control and food security. At the same time, due to people's irrational use of insecticides and the inherent shortcomings of some insecticides, a series of problems have been brought about, such as insecticide resistance, pesticide residues and poor selectivity. Therefore, finding novel, efficient and safe insecticides is a hot spot in the research and development of pesticides. Insect growth regulators (IGRs) can affect the normal growth and development of insects, resulting in incomplete metamorphosis or death of larvae, and are known as the pesticides of the 21st century. As a kind of insect neuropeptides, Allatostatins (ASTs) are small peptides composed of several to dozens of amino acids...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07K5/113A01N37/20A01N37/46A01P7/04
CPCA01N37/20A01N37/46C07K5/1021
Inventor 杨新玲汪梅子凌云开振鹏周源琳金小宇
Owner CHINA AGRI UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com