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Marbofloxacin-calcium chelate and its synthesis method and application

A calcium chelate, marbofloxacin technology, applied in the direction of calcium organic compounds, drug combinations, antibacterial drugs, etc., can solve the problems of metal complex or chelate synthesis and use that have not been published in reports, etc., Improve immunity and promote growth

Active Publication Date: 2016-05-04
GUANGXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But up to now, there is no published report on the metal complexes or chelates of marbofloxacin and their synthesis and use.

Method used

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  • Marbofloxacin-calcium chelate and its synthesis method and application
  • Marbofloxacin-calcium chelate and its synthesis method and application
  • Marbofloxacin-calcium chelate and its synthesis method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Take 3mmol of H-Marbo dissolved in 15mL of water to form a suspension; take 3mmol of triethylamine and add it dropwise to the H-Marbo suspension, stir and react at room temperature, and the solution gradually becomes clear. Add 1mmol of Ca(NO 3 ) 2 4H 2 O was dissolved in 5 mL of water, added dropwise to the above aqueous solution, stirred and reacted at room temperature for 12 hours, a large amount of precipitates formed. Filtration, the precipitate was washed with a small amount of cold water and ethanol in turn, and vacuum-dried at room temperature for 4 hours to obtain white microcrystals, which were determined to be the target chelate [Ca II (Marbo) 2 (Marbo-H + )(H 2 (0)] (yield: 75%).

Embodiment 2

[0032] Dissolve 3mmol of H-Marbo in 100mL of water to form a suspension; dissolve 3mmol of triethylamine in 10mL of water and add it to the suspension of H-Marbo, the solution gradually becomes clear. Add 1mmol of Ca(NO 3 ) 2 4H 2O was dissolved in 20 mL of water, added dropwise to the above aqueous solution, and reacted with stirring at 50°C for 5 hours. After the reaction, the aqueous solution was clear without precipitation. The reaction solution was evaporated and concentrated to about 20mL under reduced pressure to remove most of the water solvent, and then 100mL of ethanol was added to mix to precipitate the product, and a large amount of precipitate was precipitated after sufficient cooling. Filter, wash the precipitate with a small amount of cold water and ethanol in turn, and dry in vacuum at 40°C for 1 hour to obtain white microcrystals, which were determined to be the target chelate [Ca II (Marbo) 2 (Marbo-H + )(H 2 (0)] (yield: 80%).

Embodiment 3

[0034] Take 3mmol of H-Marbo and dissolve it in 80mL of water / ethanol mixed solvent (the volume ratio of water and ethanol is 1:1) to form a suspension; take 3mmol of triethylamine and add it dropwise to the mixture of H-Marbo In suspension, the solution gradually became clear. Add 1mmol of Ca(NO 3 ) 2 4H 2 O was dissolved in 10 mL of water, added dropwise to the above aqueous solution, and reacted with stirring at 60°C for 3 hours. After the reaction, the aqueous solution was clear without precipitation. The reaction solution was evaporated and concentrated to about 20 mL under reduced pressure to remove most of the solvent, and then 100 mL of ethanol was added to mix to precipitate the product, and a large amount of precipitate was precipitated after sufficient cooling. Filter, wash the precipitate with a small amount of cold water and ethanol in turn, and dry it under normal pressure at 40°C for 3 hours to obtain white microcrystals. The structure was determined by infr...

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Abstract

The invention discloses a marbofloxacin-calcium chelate and a synthetic method and application thereof. The synthetic method of the marbofloxacin-calcium chelate comprises the following steps: 1, weighing marbofloxacin and calcium nitrate according to a stoichiometric ratio, then weighing triethylamine with the equal substance amount with the marbofloxacin, and dissolving in a polar solvent; 2, performing a reaction on the obtained solution under the condition of 20 to 70 DEG C; 3, when a product exists in the reaction solution mainly in a precipitate mode, filtering the obtained reaction solution and washing and drying precipitates to obtain the target product, and when the product is mainly dissolved in the reaction solution, concentrating the obtained reaction solution to remove most of solvent, adding excessive ethanol, separating out the precipitates and washing and drying the precipitates to obtain the target product. By inspecting the in-vitro antibacteral activity and the in-vivo acute toxicity of the chelate by the applicant, a result shows that the in-vitro bacteriostasis effect of the marbofloxacin-calcium chelate is equivalent to that of the marbofloxacin, but the in-vivo acute toxicity of the marbofloxacin-calcium chelate is obviously lower than that of the marbofloxacin. The structural formula of the marbofloxacin-calcium chelate is as shown in the following formula (referring to the specification).

Description

technical field [0001] The invention relates to a metal chelate, in particular to a calcium chelate with marbofloxacin as a ligand, a synthesis method and application thereof. Background technique [0002] Quinolones, the derivatives of 4-quinolones, are an important class of organically synthesized antibacterial drugs. According to the parent ring structure, quinolones can be divided into nalidixic acids, pipemidic acids, quinolinic acids and ofloxacin. Since the advent of nalidixic acid in 1962, the development of quinolones has been very rapid, and four generations of drugs have been developed. At present, the third-generation drugs and a small amount of fourth-generation drugs are mainly used in the market. Quinolones have the advantages of broad antibacterial spectrum, high curative effect, few adverse reactions, high bioavailability, and long half-life. Based on the development of new low-toxic drugs. [0003] In recent years, by studying the antibacterial mechanism...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F3/04A61P31/04A61P37/04
Inventor 刘延成陈振锋梁宏解艳杰邓胜平
Owner GUANGXI NORMAL UNIV
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