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Application of heterocyclic acrylketone type compound as antibacterial agent

A technology of acrylone and compounds, applied in the field of medicine, can solve problems such as ineffective colistin-resistant bacteria and unknown systemic infection models

Active Publication Date: 2019-04-16
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, Jian Li et al. (Front.Microbiol.2018Apr12; 9:721) found that the combination of colistin and mitotane can produce a bactericidal effect on colistin-resistant bacteria, and can improve the skin colony of burned skin infection model mice number, but efficacy in systemic infection models remains unknown
Deng Xuming et al. (Antimicrob Agents Chemother. 2018 Mar 27; 62(4)) found that the combination of pterostilbene and colistin can produce a bactericidal effect on colistin-resistant strains carrying the mcr-1 gene, but it has a bactericidal effect on African Colistin-resistant bacteria carrying the mcr-1 gene are ineffective
Most of the research and development of polymyxin sensitizers are still in the early preclinical research stage, and no compound has entered the clinical trial stage so far

Method used

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  • Application of heterocyclic acrylketone type compound as antibacterial agent
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  • Application of heterocyclic acrylketone type compound as antibacterial agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Embodiment 1: the mensuration of compound antibacterial spectrum

[0070] According to the method recommended by CLSI, the minimum inhibitory concentration (MIC) was determined by plate double dilution method and multi-point inoculator. Compounds PFK-158, PFK-015 and 3PO of the present invention were all purchased from Shanghai Taosu Biochemical Technology Co., Ltd.; reference substances (levofloxacin, polymyxin E, polymyxin B, etc.) were all purchased from China Food and Drug Administration Research Institute of Standardization and Standardization Institute. Drugs etc. are all diluted into various required concentrations with broth twice, add appropriate amount to the plate respectively, after the agar medium is melted, pour quantitatively into the plate containing the drug solution and mix evenly, the compound of the present invention (such as the compound prepared in the examples) The final concentrations of the control substance and the reference substance were 0.0...

Embodiment 2

[0077] Example 2: Determination of compound polymyxin E combined with MIC by checkerboard method

[0078] Strains frozen at -70°C were streaked on nutrient agar plates and cultured overnight at 37°C. Pick 3 to 5 well-separated and uniformly shaped colonies from the agar petri dish and inoculate them into a small glass test tube containing 3 mL of CAMHB, and incubate at 37°C and 200 rpm for 6 to 7 hours. Take the bacterial liquid in the exponential growth phase and measure the McFarland concentration of the bacterial liquid in each test tube with a McFarland turbidimeter, and then use 0.85% NaCl solution to adjust the bacterial liquid to 0.5 McFarland, about (1~2)×10 8 CFU / mL. The bacterial solution was used within 15 minutes after preparation. Take the prepared polymyxin E and dilute it to an appropriate concentration with CAMHB for later use. Add 100 μL of CAMHB to the 96-well plate, add the same volume of the above antibiotics to the first column, and serially dilute them...

Embodiment 3

[0082] Example 3: PFK-158 combined with polymyxin E against systemic infection in mice caused by E.cloacae D01

[0083] Inoculate an appropriate amount of frozen-preserved bacteria from E.cloacae D01, a high-level polymyxin-resistant strain, into 10 mL of Zeng Bacteria Decoction, and culture it at 37°C for 6 hours. Cultivate statically at ℃ for 18 hours; the obtained bacterial liquid is properly diluted with 5% dry active yeast solution to prepare the infectious bacterial liquid for use; at the same time, it is diluted several times with 0.85% NaCl, and 10 μL is dripped on the MH plate, and left to dry Colony counting after inversion culture; female mice were randomly divided into groups according to body weight, 10 in each group; the abdomen was disinfected with iodine, and the mice were lightly inverted and intraperitoneally injected with 0.5mL of bacterial solution; 1mg / kg was prepared with 0.85% NaCl solution Polymyxin E alone and combined with 5, 10, and 15 mg / kg PFK-158 ...

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Abstract

The invention discloses application of a heterocyclic acrylketone type compound as an antibacterial agent. The compound has remarkable antibacterial activity on gram-positive bacteria; in addition, the heterocyclic acrylketone type compound and polymyxin are combined to have remarkable anti-polymyxin drug-resistance bacterium activity on gram-negative bacteria.

Description

technical field [0001] This application includes but is not limited to the field of medical technology, in particular, it relates to the use of heterocyclic propenone compounds as antibacterial agents. Background technique [0002] In 2017, the World Health Organization (WHO) released a list of key pathogens for research and development of new antibiotics, carbapenem-resistant Acinetobacter baumannii (Carbapenem- resistant Acinetobacter Baumannii, CRAB), Pseudomonas aeruginosa (Carbapenem-resistant Pseudomonas Aeruginosa, CRPA) and Enterobacteriaceae (Carbapenem-resistant Enterobacteriaceae, CRE). For this type of drug-resistant bacteria, the only available drugs are polymyxins (including colistin and polymyxin B, etc.). In 2015, the team of Academician Shen Jianzhong from China discovered that a plasmid carrying the mcr-1 gene can mediate colistin resistance. In the past three years, colistin-resistant bacteria have been found in more and more parts of the world. So far,...

Claims

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Application Information

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IPC IPC(8): A61K31/444A61K31/4709A61P31/04C07D213/50C07D401/06
CPCA61K31/444A61K31/4709A61P31/04C07D213/50C07D401/06
Inventor 游雪甫张友文胡辛欣李雪王秀坤董立民杨信怡李聪然李国庆庞晶卢曦卢芸聂彤颖
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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