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New application of rifamycin-nitroimidazole coupling molecule

A technology of nitroimidazolium and rifamycin, which is applied in the field of medicinal chemistry and can solve the problem of no documented antibacterial activity of anaerobic flora

Inactive Publication Date: 2017-06-20
TENNOR THERAPEUTICS (SUZHOU) LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] Compound 4-deoxy-3,4-[2-spirocycle-[2-(2-methyl-5-nitro-imidazol-1-yl)ethyl]-piperidine is disclosed in U.S. Patent No. 7,678,791B2 -4-yl]]-(1hydro)-imidazo-(2,5-dihydro)rifamycin S, which has antimicrobial activity against several bacteria such as Escherichia coli, but is not documented It has antimicrobial activity against anaerobic flora

Method used

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  • New application of rifamycin-nitroimidazole coupling molecule
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  • New application of rifamycin-nitroimidazole coupling molecule

Examples

Experimental program
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Effect test

Embodiment 1

[0030] This example provides the application of the rifamycin-nitroimidazole coupling molecule represented by formula I in inhibiting anaerobic bacteria;

[0031]

[0032]Among them, anaerobic bacteria include Actinomyces naeseri, Anaerobic coccus praustzii, Atobo vaginalis, Bacteroides fragilis (including metronidazole-resistant type), Bacteroides polymorpha (including metronidazole-resistant type ), Bacteroides cellulosus, Bacteroides monomorpha, Bacteroides vulgaris, Bacteroides ovale (including metronidazole-resistant types), Bifidobacterium breve, Bifidobacterium longum, Clostridium sporeformans, Perfringens Clostridium difficile (including metronidazole-resistant type), Eubacterium rectum, Fusobacterium nucleatum, Gardnerella vaginalis, Lactobacillus crispatus, Lactobacillus gasseri, Lactobacillus jansnii, Mobilis kervii, Campylobacter shy, Peptococcus (Niger), Glycopeptophilus (including metronidazole-resistant), Peptostreptococcus large, Peptostreptococcus anaerobic...

Embodiment 2

[0052] This example provides the prescription and preparation method of a fast-release oral preparation of the rifamycin-nitroimidazole conjugate molecule represented by formula I.

[0053]

[0054] Weigh the rifamycin-nitroimidazole coupling molecule and auxiliary materials represented by the formula I according to the above-mentioned prescription amount. Dissolve povidone K30 (PVP K30) and sodium dodecyl sulfate (SDS) in purified water, stir for 1 hour, and use it as an adhesive for later use; couple rifamycin-nitroimidazole shown in formula I Molecule, mannitol and carboxymethyl starch sodium (DST) are passed through a 30-mesh sieve, added to the granulator, pre-mixed, the impeller stirring speed is 700rpm, and the time is about 15 minutes. Then use a peristaltic pump to add an appropriate amount of purified water and binder to the mixture of the granulator at a fixed speed (145-165g / min). The stirring speed of the impeller of the granulator is 400rpm, and the time is ab...

Embodiment 3

[0057] This example provides a method for preparing an injection of the rifamycin-nitroimidazole conjugate molecule represented by formula I.

[0058]

[0059] Add mannitol, acetaldehyde sodium sulfoxylate, and Tween-80 to an appropriate amount of water for injection under nitrogen protection, add the rifamycin-nitroimidazole coupling molecule shown in formula I, and stir at a medium speed for 10-15 minutes. Wet the rifamycin-nitroimidazole coupling molecule shown in formula I, and slowly add 1N NaOH dropwise, which takes about 175 minutes (fast at the beginning and slow at the end), to the rifamycin-nitroimidazole shown in formula I The coupling molecules are all dissolved, filtered through two microporous membranes of 0.45+0.22 μm, the filtrate is filled into 10mL glass bottles, each bottle contains 3.5mL, the glass bottles are transferred to a freeze dryer for lyophilization, and the formula is obtained after capping The freeze-dried powder injection of the rifamycin-nit...

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Abstract

The invention discloses an application of a rifamycin-nitroimidazole coupling molecule shown in formula I in restraining anaerobic flora. The rifamycin-nitroimidazole coupling molecule shown in formula I provided by the invention has a broad-spectrum antibacterial activity to anaerobion, has an activity to most pathogenic bacteria related to bacterial vaginosis, has a better in vitro antimicrobial activity than that of bacterial vaginosis drugs, such as, metronidazole and clindamycin, and has an excellent application prospect at the aspect of preventing and treating the bacterial vaginosis or the other related diseases caused by the anaerobion.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a new application of a rifamycin-nitroimidazole coupling molecule. Background technique [0002] Anaerobic bacteria are a group of bacteria that grow better in the absence of oxygen than in aerobic environments, but cannot grow on the surface of solid media at air (18% oxygen) and / or 10% carbon dioxide concentrations . This type of bacteria lacks a complete metabolic enzyme system, and its energy metabolism is carried out by anaerobic fermentation. [0003] Anaerobic bacteria include the following categories: [0004] 1. Gram-positive anaerobic cocci (GPAC) [0005] Including Peptostreptococcus, Finegoldia, Anaerococcus, Peptoniphilus, Veillonella, etc., are the human oral cavity, upper respiratory tract, gastrointestinal tract and Part of the microbial flora of the female genitourinary system, it is an opportunistic pathogen that can cause various degrees of in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/438A61K47/54A61P15/02A61P31/04
CPCA61K31/438A61K9/0053A61K9/0019A61P15/02A61P31/04A61K9/4858A61K47/10A61K9/0014A61K9/06A61K47/32A61K47/552Y02A50/30
Inventor 马振坤袁鹰刘宇王晓梅
Owner TENNOR THERAPEUTICS (SUZHOU) LTD
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