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6,18-epoxy-14 hydroxy erythromycin lactone B and preparation method thereof

A technology of hydroxyerythromycin and lactone, which is applied in the field of new compounds, can solve the problems of reducing the efficacy of erythromycin drugs and the like

Inactive Publication Date: 2010-06-23
YUNNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, with the continuous emergence of clinical drug-resistant bacteria and the enhancement of drug resistance of these bacteria, the efficacy of clinically used erythromycin drugs is gradually decreasing, and further development of new antibiotic drugs is required

Method used

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  • 6,18-epoxy-14 hydroxy erythromycin lactone B and preparation method thereof
  • 6,18-epoxy-14 hydroxy erythromycin lactone B and preparation method thereof
  • 6,18-epoxy-14 hydroxy erythromycin lactone B and preparation method thereof

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Embodiment Construction

[0022] The preparation method of 6,18-epoxy-14 hydroxyerythromycin lactone B of the present invention consists of the following steps:

[0023] 1. Erythromycin-producing actinomycetes Actinopolyspora sp.YIM 90600 T Fermentation treatment of strains:

[0024] a. Cultivate ISP4+10% NaCl on a slant, and cultivate at 37°C for 15 days until the growth of aerial spores;

[0025] b. Seed culture ISP4 (no agar) + 10% NaCl, 37 ° C, 250 rpm, culture for 10 days;

[0026] c. Fermentation culture In the fermentation medium, at 37 degrees Celsius, 250 rpm, cultivated for 30 days, the composition and proportion of the fermentation medium: soybean powder 20g, peptone 2g, glucose 20g, starch 5g, yeast extract 2g, NaCl 74g , K 2 HPO 4 0.5g, MgSO 4 ·7H 2 O 0.5g, Na 2 SO 4 10H 2 O 25g, KCl 15g, MgCl 2 ·6H 2 O 10g, CaSO 4 2H 2 O 5g, CaCO 3 2g, 1000ml deionized water, pH 7.8;

[0027] Operation process: Take a spore of the strain that has grown in the inoculation loop, insert it i...

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Abstract

The invention relates to a new compound which is similar to a mother erythromycin nucleus but has a special structure, and a preparation method thereof. 6,18-epoxy-14 hydroxy erythromycin lactone B has the molecular formula of C21H36O8. The preparation method of the compound comprises the following steps of: firstly, the fermentation treatment of the bacterial strain of an Actinopolyspora sp. YIM 90600; and secondly, the preparation of an extract and the separation of a compound to prepare the 6,18-epoxy erythromycin lactone. The compound has the effects of anti cancer and antibiosis, and can be clinically used for treating various infections caused by sensitive bacteria. The compound can be used for synthesizing a precursor substance of a new generation of erythromycin medicines, and provides a new framework for synthesizing a new erythromycin. The structural formula of the compound is as shown in specifications.

Description

technical field [0001] The invention relates to a new compound which is similar to erythromycin core but has a unique structure, and a preparation method. Background technique [0002] Chinese patent application No. 98813253.2 discloses a "new macrolide compound", involving new erythromycin analogues and azalides, especially erythromycin with a new C-13 substituent Analogues and azalides, and pharmaceutically acceptable salts thereof. The compound is an antibacterial agent useful in the treatment of various bacterial and protozoal infections. [0003] There are many kinds of derivatives of erythromycin, and erythromycin C is used for analysis. In its 14-membered macrocyclic structure, there is no hydroxyl group at the 14th position, and no three-membered ring is formed between the 6th and 18th positions. The synthesis and development of erythromycin drugs mainly focus on the substitution of active hydroxyl groups such as 3, 5, 6, 11 and 12 on the 14-membered ring and the r...

Claims

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Application Information

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IPC IPC(8): C07D493/10C12P17/18C12P19/60C12R1/04
Inventor 赵立兴黄胜雄唐蜀昆李文均姜成林徐丽华
Owner YUNNAN UNIV