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Application of oxazolidone-nitroimidazole coupling molecule

A technology of nitroimidazoles and oxazolidinones, applied in the field of medicine, can solve problems such as lack of metabolic enzyme system, and achieve the effect of treating anaerobic bacterial infectious diseases

Inactive Publication Date: 2018-05-18
TENNOR THERAPEUTICS (SUZHOU) LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This type of bacteria lacks a complete metabolic enzyme system, and its energy metabolism is carried out by anaerobic fermentation

Method used

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  • Application of oxazolidone-nitroimidazole coupling molecule
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  • Application of oxazolidone-nitroimidazole coupling molecule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] This example provides the application of an oxazolidinone-nitroimidazole coupling molecule in anti-anaerobic Clostridium difficile, and compares and tests the in vitro antibacterial activity of a series of compounds against various bacteria. Methods as below:

[0038] 1. Materials:

[0039] Strains: as shown in Table 2. Strains were obtained from the American Type Culture Collection (ATCC). Store in a -80°C low-temperature refrigerator and resuscitate 2 days before use. Scrape a little frozen bacteria with a sterile inoculation loop, streak and inoculate on a suitable solid medium plate, and put it into a suitable gas culture environment at 35±2°C for 20-48 hours.

[0040] Table 2

[0041] bacterial species

Gram stain classification

Strain number

Enterococcus faecalis

G+

ATCC 700221

Staphylococcus aureus

G+

ATCC 29213

Klebsiella pneumoniae

G-

ATCC 43816

Acinetobacter baumannii

G-

ATCC 19606

...

Embodiment 2

[0059] This example provides an application of an oxazolidinone-nitroimidazole coupling molecule in anti-anaerobic bacteria, and at the same time tested the antibacterial activity of a series of compounds against anaerobic bacteria in vitro. Methods as below:

[0060] 1. Materials:

[0061] Strains: As shown in Table 4, 14 tested anaerobic bacteria including 13 ATCC strains and one preserved strain of Micromyx are: Bacteroides fragilis, Bifidobacterium longum, Clostridium difficile, Lactobacillus acidophilus, Egger tarda Tetrabacterium, Fusobacterium nucleatum, Gardnerella vaginalis, Animobacterium shy, Peptostreptococcus, Porphyromonas saccharolyticum, Prevotella erus, Propionibacterium acnes, Veillonella bacteria and Helicobacter pylori.

[0062] The test strains were clinically isolated Gram-positive and Gram-negative anaerobic strains deposited at Micromyx. The reference standard strains were obtained from the American Type Culture Collection (ATCC). Inoculate the stra...

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Abstract

The invention provides an oxazolidone-nitroimidazole coupling molecule, or stereoisomers, hydrates, deuterated compounds, esters, solvates, crystal forms, metabolites, pharmaceutically acceptable salts or prodrugs thereof, and application in anti-anaerobic bacteria, and belongs to the field of medicine. The oxazolidone-nitroimidazole coupling molecule has the structure shown in Formula I. The invention also provides application of the oxazolidone-nitroimidazole coupling molecule and a drug combination composition thereof in the preparation of drugs for the treatment of diseases caused by anaerobic infections. The oxazolidone-nitroimidazole coupling molecule, or stereoisomers, hydrates, deuterated compounds, esters, solvates, crystal forms, metabolites, pharmaceutically acceptable salts orthe prodrugs thereof can effectively resist anaerobic bacteria, and then treat anaerobic infections.

Description

technical field [0001] The invention relates to the application of an oxazolidinone-nitroimidazole coupling molecule and belongs to the technical field of medicine. Background technique [0002] Antibiotics are currently the first choice for humans to treat bacterial infectious diseases, but the excessive use and abuse of antibiotics has made the problem of bacterial drug resistance increasingly serious. Among them, the problem of drug resistance of Gram-positive bacteria is particularly serious, such as methicillin-resistant Staphylococcus aureus (MRSA), Staphylococcus epidermidis (MRSE), penicillin-resistant Streptococcus pneumoniae (Penicillin-resistant Streptococcus pneumoniae, PRSP) and vancomycin-resistant Enterococcus (VRE), etc., the emergence of these drug-resistant bacteria has seriously reduced the efficacy of existing drugs, resulting in long-term treatment of patients Significantly prolonged and increased mortality. [0003] Oxazolidinones are a new class of d...

Claims

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Application Information

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IPC IPC(8): C07D498/04A61K31/5365A61K31/4439A61K31/424A61K47/54A61P31/04
CPCC07D498/04Y02A50/30
Inventor 袁鹰万大维庄志军刘宇马振坤
Owner TENNOR THERAPEUTICS (SUZHOU) LTD
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