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

Application of styrene quinoline derivatives in the preparation of anti-drug-resistant bacteria drugs and anti-drug-resistant bacteria drugs

A technology of styryl quinoline and derivatives, which can be used in antibacterial drugs, resistance to vector-borne diseases, pharmaceutical formulations, etc., can solve problems such as the lag in research and development of new antibiotics

Active Publication Date: 2021-09-03
GUANGDONG UNIV OF TECH
View PDF2 Cites 0 Cited by
  • 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. Therefore, it is of great significance to develop antibacterial drugs with new mechanisms of action and new chemical structures to effectively kill drug-resistant bacteria

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
  • Application of styrene quinoline derivatives in the preparation of anti-drug-resistant bacteria drugs and anti-drug-resistant bacteria drugs
  • Application of styrene quinoline derivatives in the preparation of anti-drug-resistant bacteria drugs and anti-drug-resistant bacteria drugs
  • Application of styrene quinoline derivatives in the preparation of anti-drug-resistant bacteria drugs and anti-drug-resistant bacteria drugs

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 (...

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 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. The invention provides the application of the styrene quinoline derivatives with the structure shown in formula (I) in the preparation of drugs against drug-resistant bacteria. Positive bacteria such as Staphylococcus aureus have obvious inhibitory effect, and it also has a certain effect on negative bacteria. Through the experiment on the bacterial morphology under the action of the styrene quinoline derivative of the present invention, it can be preliminarily judged that the target of the styrene quinoline derivative of the present invention is the split protein FtsZ ubiquitous 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

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): 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
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