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Application of oxazolidinone-nitroimidazole coupling molecule

A technology of nitroimidazoles and oxazolidinones, which is applied in the field of medicine, can solve problems such as drug side effects, and achieve the effect of treating anaerobic 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

It has special curative effect on peptic ulcer infected by Helicobacter pylori and pseudomembranous colitis caused by tetracycline-resistant Clostridium difficile. The drug is the first choice for anti-anaerobic bacteria in the world, but there are also increasingly common drug-resistant bacteria and drug side effects

Method used

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  • Application of oxazolidinone-nitroimidazole coupling molecule
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  • Application of oxazolidinone-nitroimidazole coupling molecule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] This example provides an application of an oxazolidinone-nitroimidazole coupling molecule in antibacterial applications. The oxazolidinone-nitroimidazole coupling molecule is a compound represented by formula I and / or formula II:

[0024]

[0025] In this example, the compounds represented by formula I and formula II were tested for in vitro antibacterial activity of standard strains to illustrate their general antibacterial ability. For the convenience of expression, the compound shown in formula I is called compound 1 in the examples (the sample in this example is selected from batch number DJ-013-014, produced by Dannuo Pharmaceutical), and the compound shown in formula II is called compound 2 (this example Examples Sample batch number DJ-013-032, produced by Dannuo Pharmaceuticals).

[0026] In this embodiment, the in vitro antibacterial activity test on 8 standard strains was firstly used, and the 8 strains were all from the American Type Culture Collection (ATC...

Embodiment 2

[0039] This example provides an application of an oxazolidinone-nitroimidazole coupling molecule in anti-anaerobic bacteria. The oxazolidinone-nitroimidazole coupling molecule is a compound represented by formula II:

[0040]

[0041] In this example, the compound represented by formula II is called compound 2 for convenience of description (the sample in this example is selected from batch number DJ-013-032, produced by Dannuo Pharmaceutical). This example is to test the in vitro antibacterial activity of compound 2 against various ribonucleic acid types of Clostridium difficile, in order to illustrate the inhibitory effect of compound 2 on Clostridium difficile.

[0042] In this embodiment, 28 strains of Clostridium difficile were selected for testing, as shown in Table 3. Twenty-eight strains of Clostridium difficile came from the American Type Culture Collection (ATCC) and the British National Type Culture Collection (NCTC). All strains were inoculated on Brucella agar...

Embodiment 3

[0053] This example provides an application of an oxazolidinone-nitroimidazole coupling molecule in anti-anaerobic bacteria. The oxazolidinone-nitroimidazole coupling molecule is a compound represented by formula II:

[0054]

[0055] In this example, the compound represented by formula II is called compound 2 for convenience of description (the sample in this example is selected from batch number DJ-013-032, produced by Dannuo Pharmaceuticals, dissolved in DMSO). In this example, the antibacterial activity of Compound 2 against 29 different bacterial species including 20 anaerobic bacteria was tested.

[0056] The method of this embodiment is as follows:

[0057] Material:

[0058] Strains: 29 different bacterial species including: Gram-positive Enterococcus faecium, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae; Gram-negative Escherichia coli, Haemophilus influenzae, Neisseria gonorrhoeae and Mycobacterium smegmatis; ...

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Abstract

The invention provides an oxazolidinone-nitroimidazole coupling molecule or application of a stereoisomer, hydrate, a deuterium substitute, ester, solvate, a crystal form, metabolite, pharmaceuticallyaccepted salt or prodrug of the coupling molecule in resisting anaerobic bacteria. The oxazolidinone-nitroimidazole coupling molecule is a compound as shown in formula I or II. The oxazolidinone-nitroimidazole coupling molecule or the stereisomer, hydrate, deuterium substitute, ester, solvate, crystal form, metabolite, pharmaceutically accepted salt or prodrug of the coupling molecule can be usedfor effectively resisting the anaerobic bacteria and then treating anaerobic bacteria-infected diseases.

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): C07D413/12A61K31/496A61K47/54A61P31/04
CPCC07D413/12
Inventor 袁鹰丁俊刘宇马振坤
Owner TENNOR THERAPEUTICS (SUZHOU) LTD
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