Application of indol-ethylene substituted quinoline derivative in preparing drug-resistance bacterium medicines

A technology of indole ethylene and its derivatives, which can be applied in the direction of antibacterial drugs, resistance to vector-borne diseases, and pharmaceutical formulations. Toxic effects

Active Publication Date: 2018-07-24
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is still no literature report on the activity of indolevinyl substituted quinoline derivatives to inhibit the bacterial division protein FtsZ

Method used

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  • Application of indol-ethylene substituted quinoline derivative in preparing drug-resistance bacterium medicines
  • Application of indol-ethylene substituted quinoline derivative in preparing drug-resistance bacterium medicines
  • Application of indol-ethylene substituted quinoline derivative in preparing drug-resistance bacterium medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1 antibacterial activity screening

[0039] The minimum inhibitory concentration MIC (μg / mL) value of each test compound was determined by the broth microdilution method described in the Clinical and Laboratory Standards Institute (CLSI) guidelines.

[0040] 1. Test compounds are shown in Table 1, and their preparation methods have been disclosed in the following documents:

[0041] Guo Xiaolu, Design and Performance of Indolevinyl Substituted Quinoline Derivatives G-Quadruplex DNA Fluorescent Probes [D]. Guangdong University of Technology.

[0042] Table 1

[0043]

[0044] 2. Preparation of antibacterial drugs and culture medium: Dissolve the compound to be tested in DMSO to prepare a stock solution of 1.6 mg / mL, filter and sterilize for future use; sterilize the prepared MH broth medium by high-pressure steam for 30 minutes, and cool it for later use.

[0045] 3. Seed plate: measure the bacterial concentration of the bacterial suspension with a microp...

Embodiment 2

[0055] Using a microscope to observe the growth form of Bacillus subtilis under the action of indolevinyl substituted quinoline derivatives:

[0056] 1. The tested compounds are shown in Table 1, and Bacillus subtilis B.Subtilis 168 was selected as the indicator bacterium.

[0057] 2. The prepared MH broth medium was sterilized by high-pressure steam for 30 minutes, and cooled; the MH broth was diluted to a concentration equivalent to 0.5 McFarland turbidimetric tube (bacteria content 0.5×10 8 1 / mL), add 150 μL of bacterial solution to each well of the 96-well plate; the 1st column and the 12th column of the 96-well plate were not added with drugs, and were set as the blank control group; the 2nd to 9th columns of the 96-well plate were respectively Correspondingly add the stock solutions of compounds 1 to 8 prepared in Example 1, so that the concentration of each test compound is half of the MIC value in Table 2; add DMSO solvent to the 10th column in the 96-well plate as a s...

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PUM

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Abstract

The invention belongs to the technical field of medicines and in particular relates to application of an indol-ethylene substituted quinoline derivative in preparing drug-resistance bacterium medicines. The invention provides application of the indol-ethylene substituted quinoline derivative of formula (I) as shown in the specification in preparing drug-resistance bacterium medicines. The indol-ethylene substituted quinoline derivative provided by the invention has a remarkable inhibition function upon multiple drug-resistance bacteria, and is capable of remarkably inhibiting growth and propagation of vancomycin-resistant enterococcus, drug-resistant escherichia coli and methicillin-resistant staphylococcus aureus. Deep structure and function study shows that the indol-ethylene substitutedquinoline derivative provided by the invention has an action target of a bacterium split protein FtsZ, because of differences of FtsZ and human micro-tube protein sequences, drug-resistance bacteriummedicines which can selectively act upon bacteria FtsZ without interfering host cells can be designed, and the derivative is good in antibacterial activity, is capable of reducing amounts of single medicines, then reducing toxic and side effects and reducing drug resistance, and has the prospect of being developed into novel antibiotic medicines.

Description

technical field [0001] The invention belongs to the field of antibiotic drug preparation, and in particular relates to the application of indolevinyl substituted quinoline derivatives in the preparation of anti-drug-resistant bacteria drugs. Background technique [0002] 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 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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4709A61P31/04
CPCA61K31/4709Y02A50/30
Inventor 卢宇靖李莹蔡森源郑园园龙威王聪
Owner GUANGDONG UNIV OF TECH
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