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Application of a tetraphenylethylene derivative in the preparation of antibacterial drugs

A technology of tetraphenylethylene and antibacterial drugs, which is applied in the field of tetraphenylethylene derivatives in the preparation of antibacterial drugs, can solve the problems of epidemics of infectious diseases, pollution, etc., and achieve low cytotoxicity, broad application prospects, and no hemolytic side effects

Active Publication Date: 2017-05-17
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, biofilm bacteria can also contaminate equipment related to human life, such as air conditioning systems, water supply systems, and food processing equipment, which can cause the prevalence of infectious diseases

Method used

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  • Application of a tetraphenylethylene derivative in the preparation of antibacterial drugs
  • Application of a tetraphenylethylene derivative in the preparation of antibacterial drugs
  • Application of a tetraphenylethylene derivative in the preparation of antibacterial drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048]Embodiment 1: the synthesis of tetraphenylethylene derivative

[0049] Taking four-p-(p-carboxyphenyl) tetraphenylethylene as an example, its synthetic method is as follows:

[0050]

[0051] The specific steps are:

[0052] 1) Place 5g of compound 1 on the upper layer of a clean desiccator, spread about 7.5mL of bromine on the bottom of the desiccator, react for one week, dissolve the reacted solid in dichloromethane, and use methanol as a poor solvent for recrystallization. A total of 8.2 g of compound 2 was obtained by suction filtration.

[0053] 2) 644mg (1mmol) compound 2, 1.44g (8mmol) compound 3, 70mg (0.05mmol) Pd (PPh 3 ) 4 , 190mg TBAB, 5mL of 2M K 2 CO 3 The solution and 35mL THF were added into the reaction flask, heated to reflux, under nitrogen protection, and the reaction temperature was 70°C. After reacting for 48 hours, it was cooled to room temperature, washed with water three times, and the organic phase was collected. Mixed with silica gel,...

Embodiment 2

[0056] Example 2: Therapeutic effect of tetraphenylethylene derivatives on animals infected with multidrug-resistant bacteria and common bacteria

[0057] First put 10 6 CFU / mL multidrug-resistant bacteria 500 μL was injected into the abdominal cavity of mice to simulate the abdominal infection model. Normal saline was used as negative control, and vancomycin was used as positive control. Half an hour after the modeling, 100 μL of the normal saline solution of tetraphenylethylene derivatives, the negative control and the positive control were injected into the tail vein, and 100 μL was injected again 8 hours later. Observe and record the survival rate of mice. The measurement results are shown in Table 1.

[0058] Table 1

[0059]

[0060] It can be seen that in the case of all death of animals without medication, the tetraphenylethylene derivatives of 400 μg / kg dose can make the animals infected with multi-drug resistant bacteria obtain 100% survival rate, which has th...

Embodiment 3

[0062] Example 3: Inhibition of Tetraphenylethylene Derivatives to Planktonic Bacteria

[0063] The inhibitory effect of tetraphenylethylene derivatives on planktonic bacteria was expressed by the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against planktonic bacteria in vitro.

[0064] Five different bacteria S.aureus, MRSA, S.epidermidis, MRSE and B.subtilis were selected for determination. Add different concentrations of tetraphenylethylene derivatives into the five groups of bacterial culture medium, and then add the final concentration of 10 4 CFU / mL of the above-mentioned bacteria, cultured at 37°C for 24 hours and 48 hours, and observed whether the bacteria grow. The lowest concentration of tetraphenylethylene derivatives that can ensure that the bacteria do not grow is the minimum inhibitory concentration of the compound. Smear the bacterial solution with the minimum inhibitory concentration and 2 times, 4 times, and 8 times the...

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Abstract

The invention relates to an application of a tetraphenyl ethylene derivative in preparation of an antibacterial agent. The tetraphenyl ethylene derivative has a tetraphenyl ethylene structure with a substituent group on at least one benzene ring, can resist multidrug-resistant bacteria, especially can also resist planktonic bacteria and biofilm bacteria, can be used for effectively eliminating a biofilm, is low in cytotoxicity, has no hemolysis side effect, can be used for curing an animal model infected by common bacteria and multidrug-resistant bacteria and has a broad application prospect in the field of preparation of antibacterial agents.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to the use of tetraphenylethylene derivatives in the preparation of antibacterial drugs, in particular to the use of tetraphenylethylene derivatives with para-substituents on the benzene ring in the preparation of antibacterial drugs. Background technique [0002] There are many types of antibacterial drugs, including β-lactams, aminoglycosides, chloramphenicols, macrolides, glycopeptides and tetracyclines. With the use or even abuse of clinical antibacterial drugs, the problem of antimicrobial drug resistance is becoming more and more serious. In recent years, the emergence of superbugs has caused great panic among people. Therefore, the research and development of antimicrobial agents against drug resistance is still urgent. [0003] In addition to the unresolved problem of bacterial resistance, resistance to planktonic or biofilm bacteria is an unresolved problem in the field. Until the e...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/404A61K31/4425A61K31/14A61K31/085A61K31/277A61K31/194A61K38/05A61P31/04
Inventor 蒋兴宇陈雯雯
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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