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Application of benzothiazole substituted benzofuran quinoline derivative in preparation of medicament for resisting drug-resistance bacteria

A technology of benzofuranquinoline and benzothiazole, which is applied in the directions of antibacterial drugs, resistance to vector-borne diseases, pharmaceutical formulations, etc., can solve problems such as no discovery, and achieve the effect of low toxic and side effects

Active Publication Date: 2017-12-08
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 benzothiazole substituted benzofuran quinoline derivatives to inhibit the bacterial division protein FtsZ

Method used

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  • Application of benzothiazole substituted benzofuran quinoline derivative in preparation of medicament for resisting drug-resistance bacteria
  • Application of benzothiazole substituted benzofuran quinoline derivative in preparation of medicament for resisting drug-resistance bacteria
  • Application of benzothiazole substituted benzofuran quinoline derivative in preparation of medicament for resisting drug-resistance bacteria

Examples

Experimental program
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Embodiment 1

[0032] The following will clearly and completely describe the technical solutions in the embodiments of the present invention with reference to the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments are only some, not all, embodiments of the present invention. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention. Embodiment 1 antibacterial activity screening

[0033] The minimum inhibitory concentration MIC (μg / mL) value of benzothiazole substituted benzofuran quinoline derivatives was determined by micro broth dilution method.

[0034] 1. Test compounds are shown in Table 1, and their preparation methods have been disclosed in the following documents:

[0035] Wang Zhengya, benzothiazole substituted benzofuran quinoline derivatives as G-quadruplex DNA fluorescent ligan...

Embodiment 2

[0047] The growth form of Bacillus subtilis under the action of benzothiazole substituted benzofuran quinoline derivatives was observed by microscope:

[0048] 1. The tested compounds are shown in Table 1, and Bacillus subtilis B.Subtilis 168 was selected as the indicator bacterium.

[0049] 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 each / mL), add 150 μ L of bacterial solution to each hole in the 96-well plate; then, add the stock solution of the compounds 1 to 6 prepared in Example 1 respectively in the 96-well plate, so that the concentration of each test compound They are the half-value of MIC in Table 2; the blank control group uses DMSO.

[0050] Figure 1 to Figure 7In order to test the results, compared with the blank group, the bacteria in the drug-dosed group were significantly extended, and it w...

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Abstract

The invention belongs to the technical field of drugs and particularly relates to application of benzothiazole substituted benzofuran quinoline derivative in the preparation of a medicament for resisting drug-resistance bacteria. The benzothiazole substituted benzofuran quinoline derivative provided by the invention is represented by a formula (I) (shown in the description). An action target of the benzothiazole substituted benzofuran quinoline derivative is a bacteria split protein FtsZ, and the benzothiazole substituted benzofuran quinoline derivative has an obvious inhibition effect to multiple drug-resistance bacteria, is capable of obviously inhibiting the growth and propagation of vancomycin-resistant enterococcus, methicillin-resistant staphylococcus aureus and ampicillin-resistant staphylococcus aureus, has no possibility of interfering the growth of normal cells of a host and is low in toxic and side effects and hopeful of being developed into a novel antibiotic drug; a preparation method of the benzothiazole substituted benzofuran quinoline derivative is simple, wide in raw material source and low in cost and has wide market prospects.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to the application of benzothiazole-substituted benzofuran quinoline derivatives in the preparation of drugs against drug-resistant bacteria. Background technique [0002] The widespread use or even abuse of antibiotics has led to the continuous enhancement of bacterial resistance to antibiotics. Conventional antibacterial drugs are almost ineffective against drug-resistant bacteria, and the death rate caused by bacterial infections is increasing year by year. At present, many new drug-resistant bacteria (commonly known as "superbugs") have emerged one after another, such as methicillin-resistant Staphylococcus aureus (MRSA), multidrug-resistant Staphylococcus aureus (MDRSA) and vancomycin-resistant enterococci (VRE) , and there is a popular trend, there is an urgent need to develop a new type of anti-drug-resistant bacteria in clinical practice. [0003] FtsZ...

Claims

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Application Information

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IPC IPC(8): A61K31/436A61K31/5377A61K31/4545A61P31/04
CPCA61K31/436A61K31/4545A61K31/5377Y02A50/30
Inventor 郑园园卢宇靖蔡森源王聪龙威陈伟武黄玄贺
Owner GUANGDONG UNIV OF TECH
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