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Application of compound, antibacterial composition and application of antibacterial composition

An antibacterial composition and compound technology, which can be applied in the directions of active ingredients of heterocyclic compounds, antibacterial drugs, and medical preparations containing active ingredients, etc., can solve the problems of new ways of tuberculosis to be developed, and the inability to achieve good antibacterial effects in tuberculosis. , to achieve excellent antibacterial effect, strong antibacterial activity, good antibacterial effect

Active Publication Date: 2021-12-10
深圳市南山区慢性病防治院
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Combination drugs for the treatment of tuberculosis in the prior art cannot achieve good antibacterial effects, and new ways to treat tuberculosis still need to be developed

Method used

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  • Application of compound, antibacterial composition and application of antibacterial composition
  • Application of compound, antibacterial composition and application of antibacterial composition
  • Application of compound, antibacterial composition and application of antibacterial composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Compound X9 Screening

[0037] The compound library consisting of 52000 compounds of Shanghai Institute of Materia Medica was screened at Shenzhen People's Hospital.

[0038] These small compounds were screened at 2 μg / mL (mean concentration 5 to 6 μM) in the presence of 0.15 μg / mL linezolid. Each compound was prepared in 50 μL of 7H9 broth in a 96-well plate, then 50 μL of M.bovisBCG suspension was added to each well, and M.bovis BCG was grown at 37°C for two weeks.

[0039] The antibacterial activity of the compounds was determined by the resazurin reduction method, a color change from blue to pink indicated bacterial growth; DMSO was used as a positive control to define bacterial growth without any compound (100% survival), rifampicin was used Served as a negative control to kill all bacteria (0% survival); screened primarily by activity inhibition (MIC < 4 μg / mL in M. bovisBCG) and selection for drug-like properties.

[0040] The microdilution method was...

Embodiment 2

[0046] Compound X9 in Example 1 was mixed with rifampicin, linezolid and bedaquiline at a ratio of 1:1 to obtain compound X9-rifampicin composition, compound X9-linezolid composition, compound X9 - bedaquiline compositions.

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Abstract

The invention provides application of a compound, an antibacterial composition and application of the antibacterial composition and relates to the technical field of medicinal chemical industry. The compound is a compound X9, and the antibacterial composition is prepared from the compound X9 and an antituberculosis drug. According to the compound X9 provided by the invention, the problems that in the prior art, a combined medicine for treating tuberculosis cannot achieve a very good antibacterial effect, and a new way for treating the tuberculosis is lacked, are solved, the compound X9 is high in antibacterial activity, can achieve an excellent antibacterial effect at a relatively low concentration, and can achieve a synergistic antibacterial effect with rifampin, linezolid and bedaquiline. The compound X9 has relatively high binding power with a germ target protein, and is non-toxic to cells. The compound can be used for providing a new way for treating the tuberculosis, and can be combined with the existing tuberculosis medicines for treatment to achieve a better antibacterial effect.

Description

technical field [0001] The invention relates to the technical field of medicine and chemical industry, in particular to the application of a compound, an antibacterial composition and the application thereof. Background technique [0002] Tuberculosis (TB), caused by the bacterium Mycobacterium tuberculosis, is one of the most serious infectious diseases in humans, with 1.4 million deaths in 2019 (WHO). The current treatment of tuberculosis is mostly the combination therapy of isoniazid (INH), rifampicin (RIF), ethambutol (EMB) and pyrazinamide (PZA), but the combined use will cause a variety of side effects, and the tuberculosis branch Bacillus strains have also developed resistance to antibiotics. In this case, it is necessary to develop new compounds or synergists with antibacterial properties. Bedaquiline was approved as a new drug for the treatment of drug-resistant tuberculosis in 2012, which can inhibit the mycobacterium F o f 1 -ATPase (Andries K, Verhasselt P, G...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165A61K31/496A61K31/5377A61K31/47A61P31/06
CPCA61K31/165A61K31/496A61K31/5377A61K31/47A61P31/06A61K2300/00Y02A50/30
Inventor 刘盛元布丽吉特·玛丽·伊丽莎白·吉凯朱利安·雷吉·布利夫陶徐彦吉黄维郭旭君王健
Owner 深圳市南山区慢性病防治院
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