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Application of 6-dimethylaminoquinoline aromatic ethylene derivative to preparation of drugs for resisting drug-resistant bacteria

A technology of dimethylaminoquinoline aromatic vinyl and drug-resistant bacteria is applied in the directions of antibacterial drugs, resistance to vector-borne diseases, pharmaceutical formulations, etc., and can solve the problem of not finding 6-dimethylaminoquinoline aromatic vinyl derivatives and the like , to achieve the effect of reducing bacterial resistance, inhibiting growth and reproduction, and strong antibacterial activity

Active Publication Date: 2020-11-03
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 6-dimethylaminoquinoline aromatic vinyl derivatives to inhibit the bacterial division protein FtsZ

Method used

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  • Application of 6-dimethylaminoquinoline aromatic ethylene derivative to preparation of drugs for resisting drug-resistant bacteria
  • Application of 6-dimethylaminoquinoline aromatic ethylene derivative to preparation of drugs for resisting drug-resistant bacteria
  • Application of 6-dimethylaminoquinoline aromatic ethylene derivative to preparation of drugs for resisting drug-resistant bacteria

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation of Compounds 1-12

[0049] The preparation methods of compounds 1-12 (Table 1) have been disclosed in the patent (WO2006078754).

Embodiment 2

[0050] Example 2 Antibacterial activity screening

[0051] In this example, the micro broth dilution method was used to determine the minimum inhibitory concentration MIC (μg / mL) value of 6-dimethylaminoquinoline aromatic vinyl derivatives, according to the broth described in the Clinical and Laboratory Standards Institute (CLSI) guidelines The microdilution procedure determines the minimum inhibitory concentration (MIC) of the test compound. Among them, the test compounds are shown in Table 1.

[0052] Table 1 Test compounds

[0053]

[0054] The implementation steps are as follows:

[0055] (1) Preparation of culture medium and antibacterial drug stock solution: autoclave the prepared MH broth medium at 121°C for 30 minutes and then cool; dissolve the test compound in DMSO to prepare a stock solution of 3.2 mg / mL, and use 0.22 The μm membrane filter sterilizes for later use.

[0056] (2) Activation and expansion of test bacteria: spread the frozen test bacteria on a TSB agar plate,...

Embodiment 3

[0066] Example 3 Morphological study of bacteria

[0067] In this example, an Olympus IX71 inverted fluorescence microscope was used to observe the growth morphology of Bacillus subtilis under the action of the 6-dimethylaminoquinoline aromatic vinyl derivative.

[0068] The test compounds are compounds 1-12 in Table 1; the test bacteria choose B.subtilis 168; because the compound concentration is the MIC value, the growth of the bacteria is effectively inhibited, so the experimental concentration adopts 0.5×MIC to obtain a certain concentration Observe the bacterial suspension.

[0069] The implementation steps are as follows:

[0070] (1) Dilute the expanded bacterial solution with sterilized MH broth medium to a concentration of about 5×10 5 CFU / mL.

[0071] (2) Add the diluted bacterial solution and compound stock solution to the sterilized 5mL centrifuge tube, the total volume is set to 1mL, and the final concentration of the compound is the 0.5×MIC value of each compound inhibiti...

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PUM

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Abstract

The invention belongs to the technical field of drugs, and particularly relates to an application of a 6-dimethylaminoquinoline aromatic ethylene derivative to preparation of drugs for resisting drug-resistant bacteria. The 6-dimethylaminoquinoline aromatic ethylene derivative is a compound shown as a formula I or pharmaceutically acceptable salt thereof, a solvent compound, an enantiomer, a diastereoisomer and a tautomer of the compound shown as the formula I or the pharmaceutically acceptable salt thereof, or a mixture of the solvent compound, the enantiomer, the diastereoisomer and the tautomer in any proportion, and comprises a racemic mixture. The 6-dimethylamino quinoline aromatic ethylene derivative can be used as an FtsZ inhibitor, has a remarkable antibacterial effect on gram-positive bacteria and gram-negative bacteria and an effect of inhibiting bacterial division protein FtsZ, and can be used for preparing the drugs for resisting drug-resistant bacteria.(As shown in the descriptions).

Description

Technical field [0001] The invention belongs to the technical field of medicines, and specifically relates to the application of a 6-dimethylaminoquinoline aromatic vinyl derivative in the preparation of a medicine against drug-resistant bacteria. Background technique [0002] The discovery of antibiotics is one of the most breakthrough scientific achievements in the twentieth century. However, with the widespread use and even abuse of antibiotics in recent years, it has severely shortened the time required for bacteria to develop resistance and reduced humans’ resistance to bacterial infections. Ability. In 2017, the World Health Organization announced a list of pathogens that urgently need innovative treatments, including clinically multi-drug resistant Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa and various Enterobacter. The emergence of new drug-resistant bacteria has led to a decrease in the efficacy of more and more clinic...

Claims

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Application Information

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IPC IPC(8): A61K31/4709A61K31/47A61P31/04
CPCA61K31/4709A61K31/47A61P31/04Y02A50/30
Inventor 钟冬晓卢宇靖陈翠翠黄玄贺张艺瀚佘梦婷郑伯鑫龙威陈泽鑫
Owner GUANGDONG UNIV OF TECH
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