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1,1,14,14-four(2,6-dimethylphenyl)-2,13-dioxygen substitue-6,9-diammonia substitue -4,11-dihydroxy positive tetradecane compound and uses thereof

A technology of hydroxy-n-tetradecane and dimethylphenyl, applied in the field of medicine

Inactive Publication Date: 2007-09-26
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although the emergence of a variety of effective antibiotics and preventive drugs in the 20th century has rapidly reduced tuberculosis cases worldwide, it would be a big mistake to relax our vigilance

Method used

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  • 1,1,14,14-four(2,6-dimethylphenyl)-2,13-dioxygen substitue-6,9-diammonia substitue -4,11-dihydroxy positive tetradecane compound and uses thereof
  • 1,1,14,14-four(2,6-dimethylphenyl)-2,13-dioxygen substitue-6,9-diammonia substitue -4,11-dihydroxy positive tetradecane compound and uses thereof
  • 1,1,14,14-four(2,6-dimethylphenyl)-2,13-dioxygen substitue-6,9-diammonia substitue -4,11-dihydroxy positive tetradecane compound and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: 1,1,14,14-tetrakis(2,6-dimethylphenyl)-2,13-dioxo-6,9-diamino-4,11-dihydroxy-n-tetradecine Alkane compounds inhibit the growth of Mycobacterium tuberculosis in vitro:

[0036] (1) Test method:

[0037] (1) Inoculation method of Mycobacterium tuberculosis: Take 5ul of the prepared 1mg / ml Mycobacterium tuberculosis H37Ra strain bacterial suspension, and the number of bacteria contained is 1-5×10 5 , respectively inoculated in each culture tube containing 500ul 7H9 liquid medium (7H9 dry powder 4.7g / L, containing 2ml / L (v / v) glycerol and 10% ADC).

[0038](2) 1,1,14,14-tetra(2,6-dimethylphenyl)-2,13-dioxo-6,9-diamino-4,11-dihydroxy-n-tetradecane Determination of the minimum inhibitory concentration (MIC) of the compound in vitro: 1,1,14,14-tetrakis(2,6-dimethylphenyl)-2,13-dioxo-6,9-diamino- 4,11-Dihydroxy-tetradecane compound was diluted into different concentration gradients: 100μg / ml, 75μg / ml, 50μg / ml, 37.5μg / ml, 25μg / ml, 18.25μg / ml, 12.5μg / ml, 6.25μg / ml...

Embodiment 2

[0041] Example 2 The effect of shikimic acid on 1,1,14,14-tetrakis(2,6-dimethylphenyl)-2,13-dioxo-6,9-diamino-4,11-dihydroxyl Tetradecane compounds inhibit the growth of Mycobacterium tuberculosis complementation assay:

[0042] (1) Test method:

[0043] (1) Inoculation method of Mycobacterium tuberculosis: Take 5ul of the prepared 1mg / ml Mycobacterium tuberculosis suspension, containing 1-5×10 bacteria 5 , respectively inoculated in each culture tube containing 500ul 7H9 liquid medium (7H9 dry powder 4.7g / L, containing 2ml / L (v / v) glycerol and 10% ADC).

[0044] (2) After inoculating the bacteria as above and culturing them for one week, compounds with different concentration gradients (0.5ug / ml, 5ug / ml, 50ug / ml) were added to inhibit the growth of the bacteria. Add shikimic acid to the culture solution, continue to culture the bacteria for 5-6 weeks, and reach the plateau of Mycobacterium tuberculosis growth. During this process, samples were taken once a week, diluted, s...

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Abstract

The invention discloses a new compound and application to inhibit the growth of bacillus tubercle in the medical technical domain, whose chemical name is 1, 1, 14, 14-four (2, 6-dimethyl phenyl)-2, 13-dioxo-6, 9-diammonia-4, 11-dihydroxy n-tetradecane (MIC=6.25 mu g / mL).

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a new 1,1,14,14-tetrakis(2,6-dimethylphenyl)-2,13-dioxo-6, which can inhibit the growth of Mycobacterium tuberculosis. 9-diamino-4,11-dihydroxy-n-tetradecane compound and its application. Background technique [0002] Tuberculosis still poses a huge threat to mankind. Nearly 32% of the world's population has been infected with Mycobacterium tuberculosis. About 2.7 million people die from tuberculosis every year, an average of more than 7,000 people die every day. The World Health Organization declared tuberculosis a global health emergency in 1993. [0003] my country's tuberculosis epidemic is relatively serious, and it is one of the 22 countries with a high burden of tuberculosis in the world. The number of tuberculosis patients ranks second in the world. According to the analysis of the results of the fourth national tuberculosis epidemiological sampling survey...

Claims

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Application Information

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IPC IPC(8): C07C217/28A61K31/138A61P31/06
Inventor 王洪海张雪莲沈旭沈洪波赖煦卉施文钧陆静宁吴晶
Owner FUDAN UNIV
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