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Antibacterial compound containing quinoline or pyrazole heterocycle rhodanine structure

A compound, low-level technology, applied in antibacterial drugs, organic chemistry, etc., can solve problems such as increasing the difficulty of treating infectious diseases

Inactive Publication Date: 2014-02-12
YANBIAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there are many antibacterial agents used clinically and have achieved good curative effect, the long-term non-standard use of drugs has led to the emergence of various drug-resistant strains, which increases the difficulty of clinical treatment of infectious diseases

Method used

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  • Antibacterial compound containing quinoline or pyrazole heterocycle rhodanine structure
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  • Antibacterial compound containing quinoline or pyrazole heterocycle rhodanine structure

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] With (Z)-2-(5-((2-chloro-6-((4-methylbenzyl)oxy)quinolin-3-yl)methylene)-4-oxo-2-thiazolidinone Taking -3-yl)-3-phenylpropionic acid as an example to introduce the general synthesis method of compound (Ⅰ)

[0039] (1) Add 6-hydroxyquinolinone and an equivalent amount of p-methylbenzyl chloride into a 100mL round-bottomed flask, use N,N-dimethylformamide (DMF) as a solvent, add 2 times the amount of potassium carbonate, 70-80 °C for 3 hours. The reaction solution was poured into an appropriate amount of ice water, filtered, washed with water, and dried to obtain compound 3.

[0040] (2) Add 10mL DMF to a 100mL round-bottomed flask, cool it down to below 5°C with an ice-water bath, add 3g of distilled phosphorus oxychloride dropwise, and after the dropwise addition, fully stir at this temperature for 15 minutes to dissolve compound 3 Dissolve in 6 mL of DMF, add dropwise to the above mixture, stir at below 5°C for half an hour, then raise the temperature to 70°C, and st...

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PUM

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Abstract

The invention provides an antibacterial compound containing a quinoline or pyrazole heterocycle rhodanine structure and a synthetic method thereof. The antibacterial compound containing the quinoline or pyrazole heterocycle rhodanine structure has a broad antibacterial spectrum and obvious antibacterial activity on gram-positive bacteria, and minimum inhibitory concentration is 1 microgram / ml, thus the antibacterial compound containing the quinoline or pyrazole heterocycle rhodanine structure has the potential to be prepared into an antibacterial agent. The invention provides a lead compound for developing a new antibacterial agent, the synthetic method of the antibacterial compound is simple and reasonable, and production cost is low.

Description

technical field [0001] The invention provides a class of novel compounds with obvious antibacterial activity. The compound exhibits remarkable antibacterial activity against Gram-positive bacteria, and the minimum inhibitory concentration reaches 1 μg / mL. Background technique [0002] Despite the rapid progress of science and technology, the rapid development of antibacterial drugs, more than 200 kinds have been used clinically, and the lives of countless patients have been cured and saved. However, the treatment of infectious diseases is still a serious problem left to the medical field today. question. [0003] This is mainly because the current antibacterial drugs have the following problems: [0004] Antimicrobial resistance. Although many antimicrobial agents are used clinically and have achieved good curative effects, the long-term non-standard use of antibiotics has led to the emergence of various drug-resistant bacteria, which has increased the difficulty of clinic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/06C07D417/14A61K31/4709A61K31/427A61P31/04
CPCC07D417/06C07D417/14
Inventor 朴虎日郑昌吉郭萌宋明霞
Owner YANBIAN UNIV
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