Anti-infection application of thiazole-structure-containing compound

A compound and application technology, which is applied in the field of anti-infection application of compounds containing thiazole structures, can solve problems such as easy drug resistance and high pressure for bacterial survival

Active Publication Date: 2020-05-19
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional antibacterial treatment works by inhibiting or sterilizing bacteria, and bacteria are under high pressure to survive and are prone to drug resistance

Method used

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  • Anti-infection application of thiazole-structure-containing compound
  • Anti-infection application of thiazole-structure-containing compound
  • Anti-infection application of thiazole-structure-containing compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0176] Synthesis of Example 1.1 Compound ML364 (2-((4-methylphenyl)sulfonylamino)-N-(4-phenylthiazol-2-yl)-4-(trifluoromethyl)benzamide) References: Mindyl I. Davis et al., Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates cyclinD1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and MantleCell Lymphoma Models, THE JOURNAL OF BIOLOGICAL CHEMISTRY VOL.291, NO.47, pp. 24628–24640, November 18, 2016. The compounds in Table 1 can be synthesized in a similar manner.

Embodiment 12

[0177] Example 1.2 Synthesis of compound 2-((4-fluorophenyl)sulfonylamino)-N-(4-(4-isopropylphenyl)thiazol-2-yl)benzamide: same as in Example 1.1 method to synthesize the target compound.

[0178]

Embodiment 13

[0179] Synthesis of Example 1.3 Compound 2-((4-fluorophenyl)sulfonylamino)-N-(4-(4-methylphenyl)thiazol-2-yl)benzamide: obtained in Example 1.2 Intermediate 5 and Intermediate 6 were obtained in the same way as the target compound.

[0180]

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Abstract

The invention discloses anti-infection application of a thiazole-structure--containing compound. The thiazole-structure-containing compound has inhibition functions on virulence factors of pseudomonasaeruginosa of Gram-negative bacteria and virulence factors of staphylococcus aureus of Gram-positive bacteria, and ML364 in the composition is capable of increasing survival rates of mice suffering from general infection caused by carbapenem-medicine-resistant pseudomonas aeruginosa and methicillin-medicine-resistant staphylococcus aureus by 60% respectively.

Description

technical field [0001] This application relates to the field of medicine, especially but not limited to the anti-infection application of a class of compounds containing thiazole structures. Background technique [0002] Both Pseudomonas aeruginosa and Staphylococcus aureus are common pathogens of nosocomial infection, and both are prone to drug resistance. In 2017, the World Health Organization (WHO) released a list of key pathogens for the development of new antibiotics, carbapenem-resistant Pseudomonas aeruginosa (CRPA), methicillin-resistant Methicillin-resistant, vancomycin intermediate and resistant Staphylococcus aureus are extremely important (category 1 focus) and very important (category 2 focus) respectively. In order to alleviate the public health crisis caused by antibiotic resistance, it is particularly urgent to develop a new treatment strategy that is different from traditional antibacterial drugs. Traditional antibacterial treatment works by inhibiting or ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/426A61K31/427A61K31/4439A61P31/04C07D277/46C07D417/12
CPCA61K31/426A61K31/427A61K31/4439A61P31/04C07D277/46C07D417/12
Inventor 游雪甫董立民张友文李聪然杨信怡王秀坤胡辛欣聂彤颖李国庆李雪卢芸庞晶
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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