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Naproxen copper complex with function of inhibiting urease activity and preparing method thereof

A technology of urease activity and naproxen copper, which is applied in the direction of copper organic compounds, drug combinations, non-central analgesics, etc., can solve the problem of disease buried

Inactive Publication Date: 2019-07-30
NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] To sum up the reasons, thus laying a hidden danger for gastritis, gastric ulcer, gastric cancer and other diseases

Method used

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  • Naproxen copper complex with function of inhibiting urease activity and preparing method thereof
  • Naproxen copper complex with function of inhibiting urease activity and preparing method thereof
  • Naproxen copper complex with function of inhibiting urease activity and preparing method thereof

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Embodiment

[0017] The configuration of naproxen solution (0.1mmol / mL): accurately weigh 0.23g (1mmol) of naproxen and dissolve it in 10mL ethanol-acetonitrile mixed solution (ethanol:acetonitrile=1:1).

[0018] Copper nitrate solution (0.1mmol / mL) configuration: accurately weigh copper nitrate [Cu(NO 3 ) 2 ·6H 2 O] 0.1208 g (0.5 mmol) was dissolved in 5 mL of ethanol-acetonitrile mixed solution (ethanol: acetonitrile = 3: 2).

[0019] Weighing of 1,3-propylenediamine: Accurately weigh 41.67 μL (0.5 mmol) of 1,3-propylenediamine.

[0020] Accurately weigh 10 mL of naproxen solution (0.1 mmol / mL) and 5 mL of copper nitrate solution (0.1 mmol / mL) in a beaker, mix and stir at room temperature for 30 minutes, then add dropwise 1,3-propanediamine liquid (0.5 mmol) 41.67 μL, mixed and stirred at room temperature for 3 hours. Filter the reaction solution, seal it with a parafilm, prick the hole with a needle, and wait for it to stand at room temperature for slow volatilization. After a few d...

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Abstract

The invention discloses a naproxen copper complex with a function of inhibiting the urease activity and a preparing method thereof, and belongs to the technical field of complex synthesis and medicinal chemistry. According to the naproxen copper complex, naproxen and 1,3-propane diamine serve as ligands, a copper ion serves as a center ion, and through a solvent evaporation method, a mononuclear-structure naproxen copper complex is prepared. The naproxen copper complex has the good biological activity, it discovers after detection that IC50 values of the naproxen copper complex and positive control medicine acetohydroxamic acid (N-glycolamide) are 1.69 micromole / L and 6.26 micromole / L respectively with respect to urease inhibition, it indicates that an effect of the complex for inhibitingthe urease activity is better than an effect of acetohydroxamic acid, the inhibition ratio of the complex for the urease activity is 72.6%, and the naproxen copper complex is a good urease inhibitor.

Description

technical field [0001] The invention relates to a naproxen copper complex with urease-inhibiting activity, a preparation method and application thereof, and belongs to the technical field of complex synthesis and medicinal chemistry. Background technique [0002] Naproxen is a class of non-steroidal anti-inflammatory drugs, which can exert anti-inflammatory, antipyretic and analgesic effects by inhibiting the synthesis of prostaglandins. The side effects are manifested in gastrointestinal adverse reactions, such as gastric ulcer and colonic lesions. [0003] Helicobacter pylori is a Gram-negative bacillus that can survive in the strong acidic environment of the stomach. In addition to using its helical structure to penetrate the mucus on the surface of the gastric mucosa, it parasitizes in the mucus and is close to the opposite middle of the gastric mucosal epithelium. In addition to being in a sexual environment, it also benefits from the highly active urease it contains. ...

Claims

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Application Information

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IPC IPC(8): C07F1/08A61P29/00
CPCC07F1/08
Inventor 朱海亮褚怡春王甜甜杨鹏浩葛相妤李伟
Owner NANJING UNIV
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