Application of styrene quinoline derivative to preparation of drug-resistance bacteria antagonizing medicine and drug-resistance bacteria antagonizing medicine

A technology of styrene-quinoline and drug-resistant bacteria, which is applied in antibacterial drugs, resistance to vector-borne diseases, and pharmaceutical formulations. The effect of strong bacterial activity

Active Publication Date: 2019-10-08
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The development of new antibiotics is relatively lagging behind, and the problem of bacterial resistance has become one of the new challenges we are facing today. T...

Method used

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  • Application of styrene quinoline derivative to preparation of drug-resistance bacteria antagonizing medicine and drug-resistance bacteria antagonizing medicine
  • Application of styrene quinoline derivative to preparation of drug-resistance bacteria antagonizing medicine and drug-resistance bacteria antagonizing medicine
  • Application of styrene quinoline derivative to preparation of drug-resistance bacteria antagonizing medicine and drug-resistance bacteria antagonizing medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1 uses micro broth dilution method to measure the MIC (μg / mL) value of styrene quinoline derivative

[0032] Minimum inhibitory concentrations (MICs) of test compounds were determined using the broth microdilution procedure described in Clinical and Laboratory Standards Institute (CLSI) guidelines.

[0033] The test compounds are shown in Table 1, and their preparation methods are disclosed in literature (Xiao-Qin Wang, Chun-Li Xia, Shuo-Bin Chen, etc. Design, synthesis, and biological evaluation of 2-arylethenylquinoline derivatives as multifunctional agents for the treatment of Alzheimer's disease.[J].J Med Chem,2015,89 349-361).

[0034] Table 1 Test compounds

[0035]

[0036]

[0037] Proceed as follows:

[0038] 1) Preparation of antimicrobial drugs and culture medium: the test compound was dissolved in DMSO to prepare a 3.2 mg / mL stock solution, which was sterilized by filtration for use; the prepared MH broth medium was autoclaved for 30 minut...

Embodiment 2

[0050] In this example, a microscope was used to observe the growth form of Bacillus subtilis under the action of indolevinyl-substituted quinoline derivatives.

[0051] The tested compounds were compounds 1-8 in Table 1, and B. subtilis 168 was selected as the indicator bacterium.

[0052] 1) Sterilize the prepared MH broth medium by high-pressure steam for 30 minutes, and cool down; dilute the bacterial solution in the MH broth to a concentration equivalent to 0.5 McFarland turbidimetric tube (bacteria content 0.5×10 8 per mL), add the diluted bacterial liquid and the compound to the sterilized centrifuge tube to set the total volume to 200 μL, and determine the amount of the compound added according to the 0.5 times MIC value of each compound inhibiting B. subtilis 168. For example, the MIC value of compound 1 to inhibit B. subtilis 168 is 4 μg / mL, and the concentration of the compound acting on bacteria is 2 μg / mL, that is, 0.125 μL is added to 200 μL of bacterial liquid (...

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Abstract

The invention belongs to the technical field of medicines, particularly relates to an application of a styrene quinoline derivative to preparation of a drug-resistance bacteria antagonizing medicine and the drug-resistance bacteria antagonizing medicine, and provides the application of the styrene quinoline derivative with a structure as shown in a formula (I) to preparation of the drug-resistancebacteria antagonizing medicine. The styrene quinoline derivative has obvious inhibitory effects on positive bacteria such as vancomycin-resistant enterococcus and methicillin-resistant staphylococcusaureus, and has a certain interaction effect on negative bacteria. According to experiments of bacterial morphology under the action of the styrene quinoline derivative, people can preliminarily judge that an effect target of the styrene quinoline derivative is a ubiquitous division protein FtsZ in bacteria.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the application of styrene quinoline derivatives in the preparation of anti-drug-resistant bacteria medicines and the anti-drug-resistant bacteria medicines. Background technique [0002] With the widespread use of antibiotics, drug-resistant bacterial infections have gradually become the greatest threat to human health, making it urgent to find new antibacterial drugs and discover new antibacterial targets. Novel drug resistance such as methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococcus (VRE), multidrug-resistant Staphylococcus aureus (MDRSA) and polymyxin-resistant Escherichia coli (MCR-1) The emergence of bacteria has made the bacteria highly resistant to antibiotics, which seriously reduces the efficacy of commonly used antibiotics in clinical practice. The development of new antibiotics is relatively lagging behind, and the p...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61K31/4709A61K31/4706A61P31/04
CPCA61K31/4706A61K31/4709A61K31/5377A61P31/04Y02A50/30
Inventor 卢宇靖陈翠翠郑伯鑫蔡森源黄玄贺李莹龙威佘梦婷
Owner GUANGDONG UNIV OF TECH
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