5-arylamino quinolyl-7,8-dione derivative and its application in preparing antibiotic medicine

A technology of arylaminoquinoline and antibacterial drugs, which is applied in the field of drugs against methicillin-resistant Staphylococcus aureus, and can solve problems such as lack of drug treatment methods

Inactive Publication Date: 2007-06-06
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is currently no effective drug treatment for

Method used

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  • 5-arylamino quinolyl-7,8-dione derivative and its application in preparing antibiotic medicine
  • 5-arylamino quinolyl-7,8-dione derivative and its application in preparing antibiotic medicine
  • 5-arylamino quinolyl-7,8-dione derivative and its application in preparing antibiotic medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1: OX-03

[0017] Dissolve 1.45g (10mmol) of 8-hydroxyquinoline and 1.08g (10mmol) of p-methylaniline in 20ml of DMF solution, add an appropriate amount of IBX, react at room temperature (25°C-30°C) for 2h, concentrate under reduced pressure and use 20ml Ethyl acetate was extracted three times, the solvent was evaporated to dryness, and silica gel column chromatography (CH3Cl:CH3OH: 7:3) was used to obtain 0.65 g of a brownish-red solid (about 40% yield). The structure of the product was determined by IR, MMR, MS and elemental analysis data.

Embodiment 2

[0018] Example 2: GX-09

[0019] 1.45g (10mmol) of 8-hydroxyquinoline and 1.24g (10mmol) of p-methoxyaniline were dissolved in 20ml of DMF solution, an appropriate amount of IBX was added, and reacted at room temperature (25°C-30°C) for 1h, concentrated under reduced pressure and used 20ml of ethyl acetate was extracted three times, the solvent was evaporated to dryness, and then silica gel column chromatography (CH3Cl:CH3OH ratio of 7:3) was used to obtain 1.4g of a brownish red solid (about 50% yield). The structure of the product was determined by IR, MMR, MS and elemental analysis data.

Embodiment 3

[0020] Embodiment 3: GX-10

[0021] 1.45g (10mmol) of 8-hydroxyquinoline and 1.72g (10mmol) of p-bromoaniline were dissolved in 20ml of DMF solution, an appropriate amount of IBX was added, and the reaction was carried out at room temperature (25°C-30°C) for 6h. Ethyl ester was extracted three times, the solvent was evaporated to dryness, and silica gel column chromatography (CH3Cl:CH3OH ratio 7:3) was used to obtain 0.82 g of a brownish-red solid (about 25% yield). The structure of the product was determined by IR, MMR, MS and elemental analysis data.

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Abstract

The present invention discloses 5-arylamino quinolyl-7, 8-dione derivative with the chemical structure expression as shown. The present invention also relates to the synthesis and application in preparing antibiotic medicine, especially medicine for antagonizing methicillin resisting Staphylococcus aureus (MRSA), of the derivative. Experiment shows that the 5-arylamino quinolyl-7, 8-dione derivative has obvious bacteriostasis effect on some Gram positive bacteria, especially on methicillin resisting Staphylococcus aureus (MRSA), and may be used in preparing effective antibiotic medicine.

Description

technical field [0001] The invention relates to a class of 5-arylaminoquinoline-7,8-dione derivatives and their application in the preparation of antimicrobial drugs, especially drugs against methicillin-resistant Staphylococcus aureus (MRSA). Background technique [0002] Antibacterial drugs are currently the most commonly used class of drugs for the treatment of bacterial infections. Over the years, with the popularization and application of antibiotics around the world, as well as serious irrational abuse, a variety of drug-resistant strains have emerged in both Gram-positive and Gram-negative bacteria. Among them, the problem of drug resistance of Gram-positive bacteria is particularly serious. Methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE) appearing worldwide, Penicillin-resistant Streptococcus pneumoniae (PRSP) and vancomycin-resistant Enterococci (VRE) are the main problems in current clinical practice. Currently, there is a...

Claims

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Application Information

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IPC IPC(8): C07D215/38A61K31/47A61K9/00A61P31/04
Inventor 杜志云黄宝华张焜方岩雄赵肃清周丽华郑杰霍延平
Owner GUANGDONG UNIV OF TECH
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