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A kind of antibacterial amidine oligomer with anti-drug resistance and its preparation method and application

A production method and oligomer-like technology, which can be used in antibacterial drugs, resistance to vector-borne diseases, organic chemistry, etc., can solve the problems of large side effects, high cytotoxicity and hemolytic activity of antibacterial polymers, etc.

Active Publication Date: 2021-04-02
HUNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the similarity in the structure of bacterial cell membranes and mammalian cell membranes endows antimicrobial polymers with high cytotoxicity and hemolytic activity, resulting in greater side effects
Therefore, to date there are no FDA-approved antimicrobial polymers for the treatment of bacterial infections

Method used

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  • A kind of antibacterial amidine oligomer with anti-drug resistance and its preparation method and application
  • A kind of antibacterial amidine oligomer with anti-drug resistance and its preparation method and application
  • A kind of antibacterial amidine oligomer with anti-drug resistance and its preparation method and application

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Experimental program
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Effect test

Embodiment 1

[0041] After testing, the present invention has developed 8 antibacterial amidine oligomers with broad-spectrum antibacterial properties, and its chemical formula is as follows:

[0042]

[0043] where 5≤n≤8;

[0044] Wherein the molecular formula of R is as shown in formula (I), formula (II), formula (III), formula (IV), formula (V), formula (VI), formula (VII) or formula (VIII);

[0045]

[0046]

[0047] For convenience of record, the molecular formula of R is the compound when formula (I), formula (II), formula (III), formula (IV), formula (V), formula (VI), formula (VII) and formula (VIII) They are respectively numbered as PBAM-1, PBAM-2, PBAM-3, PBAM-4, PBAM-5, PBAM-6, PBAM-7, PBAM-8. The antibacterial properties of the 8 compounds are shown in Table 1 and Table 2:

[0048] Antibacterial properties of 8 kinds of compounds in table 1

[0049]

[0050]

[0051] Antibacterial properties of 8 compounds in table 2

[0052]

[0053]

[0054]in, a Indic...

Embodiment 2

[0070] In order to expand the types of antibacterial amidine oligomers, different H 2 N-R-NH 2 As a mixed raw material to prepare antibacterial amidine oligomers, it is found that the obtained mixed product also has obvious antibacterial properties, as shown in Table 3:

[0071] Table 3 Mixed raw materials prepare the antibacterial properties of antibacterial amidine oligomers

[0072]

[0073]

[0074] Table 3 shows that the R group of the antibacterial amidine oligomer is a mixed group and also has antibacterial properties.

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Abstract

The invention discloses an antibacterial amidine oligomer with drug resistance and its preparation method and application. The antibacterial species of the amidine oligomer include Bacillus subtilis, Escherichia coli, Enterococcus faecalis, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter cloacae. The structure disclosed by the invention has dual antibacterial mechanisms of destroying cell membranes and binding chromosomal DNA, has the characteristics of rapid sterilization and drug resistance, and exhibits broad-spectrum antibacterial properties. In addition, the structure utilizes the difference between bacteria without a nucleus and bacteria with a nucleus, and specifically targets the DNA of bacteria, significantly reducing its cytotoxicity and improving its therapeutic index.

Description

technical field [0001] The invention relates to the field of medicine and chemical industry, and more specifically relates to an antibacterial amidine oligomer with anti-drug resistance and its preparation method and application. Background technique [0002] Antibiotic resistance has gradually become a new threat to human healthcare. Recently, we have established the concept of anti-drug resistance antimicrobials, aiming to address this huge threat by reducing the rate of development of drug resistance. [0003] The antimicrobial agent with anti-drug resistance should have the following characteristics: 1) The rate of bacterial resistance to it during drug treatment is low; 2) It has a good killing effect on pathogens with multi-drug resistance. It is well known that the root cause of antibiotic resistance is the mutation of its targets, which renders drugs with different mechanisms of action ineffective. Therefore, if a drug can target multiple targets, or its targets in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C257/18C07C323/41C07C319/20A61P31/04
CPCA61P31/04C07C257/18C07C319/20C07C323/41Y02A50/30
Inventor 白玉罡冯欣欣白思蕾杨凯玲王建雪
Owner HUNAN UNIV
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