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Application of a 6-dimethylaminoquinoline aromatic vinyl derivative in the preparation of anti-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 inhibiting growth and reproduction and having a broad antibacterial spectrum

Active Publication Date: 2022-07-05
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 a 6-dimethylaminoquinoline aromatic vinyl derivative in the preparation of anti-drug resistant bacteria
  • Application of a 6-dimethylaminoquinoline aromatic vinyl derivative in the preparation of anti-drug resistant bacteria
  • Application of a 6-dimethylaminoquinoline aromatic vinyl derivative in the preparation of anti-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 to 12 (Table 1) have been disclosed in the patent (WO2006078754).

Embodiment 2

[0050] Example 2 Antibacterial activity screening

[0051] In this example, the microbroth 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 Minimal inhibitory concentrations (MICs) of test compounds were determined by a microdilution procedure. 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: The prepared MH broth was cultured based on autoclaving at 121 °C for 30 min and then cooled; the test compound was dissolved in DMSO to prepare a 3.2 mg / mL stock solution, and 0.22 Sterilized by filtration with a μm filter.

[0056] (2) Activation and expanded culture of test bacteria: Spread the cryopreserved ...

Embodiment 3

[0066] Example 3 Study on bacterial morphology

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

[0068] The test compounds are compounds 1 to 12 in Table 1; B. subtilis 168 was selected as the test bacteria; since the growth of bacteria was effectively inhibited when the compound concentration was the MIC value, the experimental concentration was 0.5 × MIC to obtain a certain concentration of Bacterial suspension observation.

[0069] The implementation steps are as follows:

[0070] (1) Dilute the expanded bacterial solution with sterilized MH broth 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 as 1mL, and the final compound concentration is 0.5×MIC value of each compound inhibit...

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Abstract

The invention belongs to the technical field of medicines, and in particular relates to the application of a 6-dimethylaminoquinoline aromatic vinyl derivative in the preparation of anti-drug resistance medicines. Described 6-dimethylaminoquinoline aromatic vinyl derivative is formula I compound or its pharmaceutically acceptable salt, and the solvate, enantiomer of described formula I compound or its pharmaceutically acceptable salt isomers, diastereomers, tautomers or mixtures thereof in any ratio, including racemic mixtures; this 6-dimethylaminoquinoline aromatic vinyl derivative can be used as an FtsZ inhibitor, which is gram-positive Bacteria and Gram-negative bacteria have significant bacteriostatic effect and the effect of inhibiting bacterial division protein FtsZ, and can be used to prepare anti-drug-resistant bacteria.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the application of a 6-dimethylaminoquinoline aromatic vinyl derivative in the preparation of anti-drug resistance medicines. Background technique [0002] The discovery of antibiotics is one of the most groundbreaking scientific achievements of the twentieth century, but with the widespread use and even abuse of antibiotics in recent years, the time it takes for bacteria to develop drug resistance has been severely shortened, and the human resistance to bacterial infections has been greatly reduced. Ability. The list of pathogens in urgent need of innovative treatments announced by the World Health Organization in 2017 includes clinically multidrug-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 mo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4709A61K31/47A61P31/04
CPCA61K31/4709A61K31/47A61P31/04Y02A50/30
Inventor 颜金武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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