Application of aminoglycoside antibiotic in preparing pharmaceutical composition for treating drug-fast bacteria infection

A technology of aminoglycosides and antibiotics, which is applied in the direction of sugar derivatives, antibacterial drugs, drug delivery, etc., and can solve the problems of not being able to cover the invention concept

Active Publication Date: 2008-04-02
CHANGZHOU FANGYUAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, the above-mentioned patent documents cannot cover the inventive concept of this patent

Method used

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  • Application of aminoglycoside antibiotic in preparing pharmaceutical composition for treating drug-fast bacteria infection
  • Application of aminoglycoside antibiotic in preparing pharmaceutical composition for treating drug-fast bacteria infection
  • Application of aminoglycoside antibiotic in preparing pharmaceutical composition for treating drug-fast bacteria infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0124] Embodiment 1: Synthesis of 1-N-(S)-3-amino-2-hydroxypropionyl gentamicin C1a

[0125] 1) Synthesis of 3, 2', 6'-tri-N-formyl gentamycin C1a

[0126] 25 grams of gentamicin C1a (GMC1a) was dissolved with 500 mL of dimethyl sulfoxide (DMSO) under stirring, cooled to room temperature, 100 mL of dichloromethane and 32 grams of cobalt acetate tetrahydrate were added, stirred and dissolved at room temperature and complexed. Add 40 g of 2-formylmercaptothiazole in batches, and react for 1 hour under stirring. Add 500mL of 5°C cold water to the reaction solution and mix evenly, separate the liquids, add 5 grams of activated carbon to the upper layer and stir for 20 minutes to filter, and the filtrate is extracted with 1 / 10 of the volume of the filtrate with dichloromethane, and extracted twice.

[0127] The upper aqueous phase was dynamically adsorbed by an 800mL HD-2 resin (ammonium type) column, washed with water to remove DMSO, and then eluted with 0.4N ammonia water. When ...

Embodiment 2

[0134] Example 2: Synthesis of 1-N-(S)-3-amino-2-hydroxypropionyl-3″-N-demethylgentamycin C1a

[0135] Add 20 mL of water and 100 mL of DMSO to 5 grams of 3″-N-demethylgentamycin C1a, stir to dissolve, add 10 grams of zinc acetate to dissolve, and add 8.5 grams of 2-formylmercaptothiazole in batches at room temperature to react. Reaction Add 150mL of cold water to the liquid, mix well, and filter. The filtrate is dynamically adsorbed with weakly acidic cationic resin D151, washed with water, and eluted with 0.4N ammonia water. When the pH is 9.5, it begins to collect in sections. The same components are combined, evaporated to dryness under reduced pressure, and obtained Solid 3.5 g.

[0136] The above solid was subjected to 1-N acylation reaction and purified by the method of step 2) in Example 1 to obtain 1-N-(S)-3-amino-2-hydroxypropionyl-3″-N-demethylated Qingda Mycin C1a base 1.8 g.

[0137] Take 1.5 grams of the above-mentioned solids and dissolve them in 30 mL of wate...

Embodiment 3

[0138] Example 3: Synthesis of 1-N-(S)-3-amino-2-hydroxypropionyl-3″-N-demethylgentamycin C1a

[0139] 8 g of 1-N-(S)-3-amino-2-hydroxypropionyl gentamicin C1a sulfate was dissolved in 100 mL of water, 10 g of sodium acetate was added, and 10 g of iodine was added dropwise (dissolved in 100 mL of dimethylformamide ), stirred and reacted at 50-70° C. for 12 hours. The reaction solution was diluted with water to 400mL, dynamically adsorbed with 100mL D151 resin, washed with water, and eluted with 0.4N ammonia water. When the pH was 9.5, it began to be collected in sections. The same components were combined and evaporated to dryness under reduced pressure. Add 50 mL of water to dissolve, purify with HD-2 (weakly acidic cationic resin) resin column (height / diameter > 10), elute with 0-0.4N ammonia water, and collect in sections. Combine the same components, concentrate to dryness, dissolve with 30mL water, add 6N H 2 SO 4 Adjust the pH to 4.5-7, add 1 gram of activated carbon ...

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Abstract

The invention provies an application of an aminoglycoside antibiotic in preparing drug combination to treat drug-resistant bacteria infection, belonging to the aminoglycoside antibiotic application technical field. The invention provides the application method of 2'-NH2-3',4'-dideoxy aminoglycoside antibiotic1-N-acyl derivatives and the preparation methods of the derivatives and agents of the product.

Description

technical field [0001] The application of an aminoglycoside antibiotic in the preparation of a pharmaceutical composition for treating drug-resistant bacterial infection belongs to the technical field of aminoglycoside antibiotic application. The present invention relates to having 2'-NH 2 1-N-acylated derivatives of aminoglycoside antibiotics with 3', 4'-dideoxy structures and their application in the preparation of pharmaceutical compositions against drug-resistant bacteria. Background technique [0002] Document 1CN1420120A, [0003] Document 2ZL93112412.3, [0004] Document 3ZL01133701.X, [0005] Document 4USP4117221, [0006] Document 5USP4230847, [0007] Document 6USP5442047. [0008] Since the listing of aminoglycoside antibiotics, their broad-spectrum antibacterial activity, especially against Gram-negative bacteria, has a good synergistic effect with β-lactam antibiotics widely used in clinical practice and their main otic , Renal toxicity is predictable, t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7036A61K9/00A61K9/08A61K9/12A61K9/20A61P31/04C07H15/226
CPCA61K31/7036A61P31/04
Inventor 刘军
Owner CHANGZHOU FANGYUAN PHARMA
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