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Novel fusidic acid derivative, preparation method and medical application thereof

A technology of fusidic acid and derivatives, which is applied in the field of new fusidic acid derivatives and their preparation, and medical applications, and can solve problems such as emulsification, impact on safety and convenience of clinical use, and precipitation

Inactive Publication Date: 2011-08-03
BEIJING RUNDEKANG MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, emulsification and precipitation often occur during use, and must be discarded immediately, seriously affecting the safety and convenience of clinical use

Method used

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  • Novel fusidic acid derivative, preparation method and medical application thereof
  • Novel fusidic acid derivative, preparation method and medical application thereof
  • Novel fusidic acid derivative, preparation method and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Dissolve 20 g of sodium fusidate in 200 ml of water, add dropwise 2N hydrochloric acid to adjust the pH to 2.0, filter, wash with water, and dry under reduced pressure at 70°C overnight to obtain 18.8 g of fusidic acid.

[0017] Weigh 10 g of fusidic acid, dissolve it in 150 ml of absolute ethanol, add 3.37 g to 15 ml of L-arginine aqueous solution under stirring, and stir at room temperature for 2 h. Filter, wash with ethanol, and dry under reduced pressure at 50°C to obtain 11.6 g of L-arginine fusidic acid. Elemental analysis C37H62N408 calculated value (%): C 64.32, H 9.04, N 8.11; measured value (%): C 64.18, H 9.12, N 7.96.

Embodiment 2

[0019] Weigh 10g of fusidic acid, dissolve it in 100ml of absolute ethanol, add 2.8g-5ml of L-lysine aqueous solution under stirring, and stir at room temperature for 2h. Filter, wash with ethanol, and dry under reduced pressure at 50°C to obtain 10.7 g of L-lysine fusidic acid. Elemental analysis C37H62N208 calculated value (%): C 67.04, H 9.43, N 4.23; measured value (%): C 67.22, H 9.28, N 4.16.

Embodiment 3

[0021] Referring to the method of Example 2, DL-lysine was used instead of L-lysine to prepare DL-lysine fusidic acid. Calcd (%) for C37H62N208: C 67.04, H 9.43, N 4.23; Found (%): C 67.28, H 9.15, N 4.08.

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Abstract

The invention provides a novel fusidic acid derivative shown in the following formula, wherein R represents basic amino acid residues such as lysines and arginines and can be of L-configuration, D-configuration or DL-configuration. The novel fusidic acid derivative shown in the formula can be used for preparing medicines for treating fusidic acid sensitized bacterial inflection.

Description

technical field [0001] The invention relates to a novel fusidic acid derivative, a preparation method and a medical application thereof. Background technique [0002] Sodium fusidate is an antibiotic with a steroidal skeleton, which produces a bactericidal effect by inhibiting bacterial protein synthesis, and has a strong antibacterial effect on a series of Gram-positive bacteria. Staphylococci, including strains resistant to penicillin, methicillin and other antibiotics, are highly sensitive to this product. There is no cross-resistance between sodium fusidate and other clinically used antimicrobials. [0003] Sodium fusidate needs to be dissolved in the attached sterile buffer solution during clinical use, and then diluted with sodium chloride injection or 5% glucose injection to 250-500 ml for intravenous infusion. The infusion time of each bottle should not be less than 2-4 hours. However, emulsification and precipitation often occur during use, and must be discarded ...

Claims

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Application Information

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IPC IPC(8): C07J13/00C07C229/26C07C279/14A61K31/56A61P31/04
Inventor 姚勇敢
Owner BEIJING RUNDEKANG MEDICAL TECH CO LTD
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