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Rare earth metal complexes using orbifloxacin as ligand, method for synthesizing same and application thereof

A technology of rare earth metals and orbifloxacin, which is applied in the fields of pharmaceutical formulations, organic active ingredients, and medical preparations containing active ingredients, etc., and can solve the problems that there are no public research reports on the synthesis of metal complexes of orbifloxacin

Inactive Publication Date: 2010-09-01
GUANGXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But at present, there is no public research report on the synthesis and application of metal complexes of orbifloxacin

Method used

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  • Rare earth metal complexes using orbifloxacin as ligand, method for synthesizing same and application thereof
  • Rare earth metal complexes using orbifloxacin as ligand, method for synthesizing same and application thereof
  • Rare earth metal complexes using orbifloxacin as ligand, method for synthesizing same and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1: Synthesis of Orbi-Nd (III) complex by solution method:

[0033] Dissolve 4mmol of H-Orbi in 100mL of water to form a suspension (suspension due to the low solubility of H-Orbi in water); dissolve 4mmol of NaOH in 10mL of water and add to the aqueous suspension of H-Orbi , the solution gradually became clear, indicating that Orbi had been converted to the sodium salt form. Then take 1mmol of NdCl 3 .6H 2 O was dissolved in 10 mL of water, added dropwise to the above aqueous solution, and mixed and reacted at room temperature for 6 hours. After the reaction, the aqueous solution was clear without precipitation. Under the condition of 70°C, most of the water solvent was distilled off under reduced pressure, and about 100mL of ethanol was added to the remaining mother liquor, and a large amount of precipitates formed. Filter, wash the precipitate with 30 mL of ethanol, and dry it under vacuum at 40°C to obtain a light green solid, which was determined to b...

Embodiment 2

[0034] Embodiment 2: Synthesize Orbi-Er (III) complex with solution method:

[0035] Dissolve 4mmol of H-Orbi in 100mL of water to form a suspension; dissolve 4mmol of NaOH in 10mL of water and add it to the aqueous suspension of H-Orbi. The solution gradually becomes clear, indicating that Orbi has been transformed into a sodium salt. form. Then take 1mmol of ErCl 3 .6H2 O was dissolved in 10 mL of water, added dropwise to the above aqueous solution, and mixed and reacted at room temperature for 2 hours. After the reaction, a large amount of precipitate was formed. After filtering, the precipitate was washed successively with 30 mL of water and 30 mL of ethanol, and dried under vacuum at 40°C to obtain a pale pink solid, which was determined to be an Orbi-Er(III) complex by infrared spectroscopy and elemental analysis, with the molecular formula [Er III (Orbi) 3 (Orbi-H + )].

Embodiment 3

[0036] Embodiment 3: Synthesis of Orbi-Sm (III) complex by solution method:

[0037] Dissolve 4mmol of H-Orbi in 100mL of water to form a suspension; dissolve 4mmol of NaOH in 10mL of water and add it to the aqueous suspension of H-Orbi. The solution gradually becomes clear, indicating that Orbi has been transformed into a sodium salt. form. Then take 1mmol of SmCl 3 .6H 2 O was dissolved in 10 mL of water, added dropwise to the above aqueous solution, and mixed and reacted at room temperature for 1 hour. After the reaction, a large amount of precipitate was formed. After filtering, the precipitate was washed successively with 30mL water and 30mL ethanol, and dried under vacuum at 40°C to obtain a light yellow solid, which was determined to be the product Orbi-Sm(III) complex by infrared spectroscopy and elemental analysis, with the molecular formula [Sm III (Orbi) 3 (Orbi-H + )].

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Abstract

The invention discloses rare earth metal complexes using orbifloxacin as a ligand, a method for synthesizing the same and application thereof. In the tests of the inhibiting effect of the complexes on bacteria such as salmonella pullorum, swine streptococcosis and bovine streptococcus uberis, the results show that the complexes have quite high bacteriostatic activity, wherein all of Er(III), Sm(III) and Eu(III) complexes of the orbifloxacin have certain bacteriostatic activity on the swine streptococcosis which cannot be inhibited by orbifloxacin and doxycycline. Mouse acute toxicity tests show that the complexes have low in-vivo toxicity to mice and are highly tolerable to mice. The toxicity of various complexes meets the acute oral toxicity ungraded standards of European Community and the PRC food security assessment grade-two (actually non-toxic) standard, wherein the neodymium complex of the orbifloxacin has the lowest toxicity.

Description

technical field [0001] The invention relates to a metal coordination compound, in particular to a rare earth metal complex with orbifloxacin as a ligand; the invention also relates to a synthesis method and application of the rare earth metal complex. Background technique [0002] Quinolones, derivatives of 4-quinolones, are an important class of synthetic 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 in recent years, and it has now developed to the fourth generation of drugs. Quinolones have the advantages of broad antibacterial spectrum, high curative effect, few adverse reactions, high bioavailability, and long half-life; however, with their wide clinical application, the problem of drug resistance has become more prominent. How to solve the problem of quinolones The ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D407/04A61K31/496A61P31/04
Inventor 梁宏陈振锋刘延成邓胜平黄遥
Owner GUANGXI NORMAL UNIV
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