Application of pyrazol compound as mycobacterium tuberculosis inhibitor

A technology for Mycobacterium tuberculosis and Mycobacterium tuberculosis is applied in the directions of antibacterial drugs, medical preparations containing active ingredients, organic active ingredients, etc. simple structure

Inactive Publication Date: 2013-05-29
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This situation has been exacerbated by the emergence of drug-resistant strains in recent years and the problem of co-infection with HIV

Method used

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  • Application of pyrazol compound as mycobacterium tuberculosis inhibitor
  • Application of pyrazol compound as mycobacterium tuberculosis inhibitor
  • Application of pyrazol compound as mycobacterium tuberculosis inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] The cultivation of embodiment 1 bacterial strain and the preparation of liquid inhibitor

[0018] Preparation of test strains:

[0019] The participating bacterial strains of this embodiment are publicly reported bacterial strains: Mycobacterium smegmatis strains (strain number: 93202; obtain from China Medical Bacteria Collection Management Center, website: http: / / www.cmccb.org.cn / , ( The same below)), Mycobacterium bovis strain (strain number: 93006, obtained from China Medical Bacteria Collection Management Center), Mycobacterium tuberculosis strain (strain number: 93004, obtained from China Medical Bacteria Collection Management Center).

[0020] Components and preparation of screening medium:

[0021] Components of the liquid screening medium and its preparation method: Add 90 ml of commercially available 7H9 liquid medium (the 7H9 liquid medium was purchased from BD Company, USA, item number: 271310) and 10 ml of OADC nutrient solution into 100 ml of liquid scree...

Embodiment 2

[0027] The in vitro bacteriostatic activity test of embodiment 2 inhibitor

[0028] According to the aseptic procedure of Example 1, the Mycobacterium tuberculosis bacterium liquid (bacteria number: 93004) of Example 1 was inoculated into the screening medium added with Inhibitor 51# to determine the in vitro effect of Inhibitor 51#. Bacteriostatic activity. In this embodiment, 50 μg / ml inhibitor 51# was added to the bacterial culture of Mycobacterium tuberculosis and cultivated at 37°C for 7-8 days. By reading each OD value and comparing with the control (including control 1 and control 2) Comparisons were made to determine whether M. tuberculosis growth was inhibited. Control 1 was without adding inhibitor 51#, and control 2 was adding rifampicin 50 μg / ml. The data during the experiment was compared with the two controls to evaluate the inhibitory effect of inhibitor 51# on Mycobacterium tuberculosis, bovine mycobacterium Bacillus strain (bacteria numbering is: 93006), the...

Embodiment 3

[0029] Embodiment 3 Determine the in vitro antibacterial activity of pyrazole compounds

[0030]Inoculate the Mycobacterium tuberculosis (strain number: 93004) bacterial liquid into the liquid screening medium supplemented with pyrazole compounds to determine the in vitro antibacterial activity of pyrazole compounds. The specific method is: the inhibitor 51# obtained by screening in Example 2 is added to the bacterial culture of Mycobacterium tuberculosis at 50 μg / ml (concentration of bacterial solution is 1~2×10 7 ) were cultured at 37°C, and after 8 days of inhibitor 51# treatment, 10 μl of Mycobacterium tuberculosis bacterial liquid was applied to the solid screening medium and cultured at 37°C for one month, and the growth of each sample was observed. The result shows: add the two samples of inhibitor 51# group and rifampicin group and all do not have single bacterium colony growth, but do not grow well without the mycobacterium tuberculosis of inhibitor 51# group, the res...

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Abstract

The invention belongs to the technical field of drug targets and in particular relates to application of a small molecular lead compound with inhibiting effect on mycobacterium tuberculosis. The small molecular compound is a pyrazol compound, with a chemical name being 2-({[1-(4-methylphenyl)-1H-pyrazol-4-yl]methyl}amino)ethanol. The compound has the advantages of small molecular weight, simple structure, good permeability and the like and can effectively inhibit growth of mycobacterium tuberculosis. Mycobacterium tuberculosis is a pathogenic bacterium of tuberculosis, so the small molecular compound has the potential of treating tuberculosis and is expected to be developed into a new antituberculosis drug. Therefore, the small molecular compound can be developed as a new antituberculosis drug and provides a new approach for treatment and cure of tuberculosis. The invention also relates to application of preparations containing the small molecular inhibitor to preparation of antituberculosis drugs.

Description

technical field [0001] The invention belongs to the technical field of screening antibacterial drugs. It specifically relates to the application of a small molecular compound specifically inhibiting the growth of Mycobacterium tuberculosis, that is, a pyrazole compound, as an anti-Mycobacterium tuberculosis inhibitor. Background technique [0002] Mycobacterium tuberculosis is a pathogen that seriously endangers human health. After Mycobacterium tuberculosis infects the human body, it will exist in the human body for several months or years. According to the statistics of the World Health Organization, about three million people die from tuberculosis every year in the world, and about one-third of the world's population is infected with latent Mycobacterium tuberculosis (WHO, 2009). Currently, TB chemotherapy consists of a mixture of first-line and second-line drugs. Actual TB treatment requires a complex and long-term regimen of 4-5 drugs over a period of 6-9 months to er...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/415A61P31/06
Inventor 何正国崔涛曾菊梅
Owner HUAZHONG AGRI UNIV
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