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Application of Vilanterol in preparation of anti-coronavirus medicine and medicine

A coronavirus, sars-cov-2 technology, used in antiviral agents, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve problems such as lack of effective prevention and treatment drugs

Pending Publication Date: 2022-06-14
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The present invention aims at the lack of effective prevention and treatment drugs for lung, respiratory and intestinal diseases, nervous system symptoms and myocarditis and other related inflammatory diseases caused by coronavirus, and points out that Vilanterol and its pharmaceutically acceptable salts are used in the preparation of anti-coronavirus inflammatory drugs Applications

Method used

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  • Application of Vilanterol in preparation of anti-coronavirus medicine and medicine
  • Application of Vilanterol in preparation of anti-coronavirus medicine and medicine
  • Application of Vilanterol in preparation of anti-coronavirus medicine and medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Fluorescence intensity changes with time of substrate peptide under papain-like protease metabolism under the action of different concentrations of Vilanterol

[0029] The specific implementation process is as follows:

[0030] 1) SARS-CoV-2 papain-like protease and substrate peptide stock solutions were stored in a -80°C refrigerator;

[0031] 2) Thaw SARS-CoV-2 papain-like protease in a freezing plate (-4 to 4°C) at room temperature, dilute 1uL in 98uL borax buffer (PH=7.4), and add it to the detection plate;

[0032] 3) Add 1 uL of inhibitors of different concentrations (compounds 1-3, the concentrations are 0, 0.025 mM, 0.25 mM, 1 mM, 2.5 mM) into the solution obtained in the above step (2);

[0033] 4) Add 1 uL of the same concentration of substrate peptide (0.5mM) to the solution obtained in the above step (3), incubate at 37°C using a fluorescence microplate reader, and use a fluorescence microplate reader to monitor the excitation at 342nm and the fl...

Embodiment 2

[0035] Embodiment 2: the inhibitory ability of compound Vilanterol to novel coronavirus papain-like protease The specific implementation process is as follows:

[0036] 1) SARS-CoV-2 papain-like protease and substrate peptide stock solutions were stored in a -80°C refrigerator;

[0037] 2) Thaw SARS-CoV-2 papain-like protease in a freezing plate (-4 to 4°C) at room temperature, dilute 1uL in 98uL borax buffer (PH=7.4), and add it to the detection plate;

[0038] 3) Add 1 uL of inhibitors of different concentrations (compound 1, the concentration is 0, 0.025 mM, 0.1 mM, 0.25 mM, 0.5 mM, 1 mM, 2.5 mM) to the solution obtained in the above step (2);

[0039] 4) Add 1 uL of the same concentration of substrate peptide (0.5mM) to the solution obtained in the above step (3), incubate at 37°C using a fluorescence microplate reader, and use a fluorescence microplate reader to monitor the excitation at 342nm and the fluorescence emission at 496nm. , detected while incubating, incubated f...

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Abstract

The invention belongs to the technical field of medicinal chemistry, and particularly relates to application of Vilanterol in preparation of a medicament for resisting coronavirus infection. According to the application, a new function of the Vilanterol is found, and the Vilanterol has a relatively strong inhibition effect on the enzymatic activity of target papaya-like protease Plpro of the coronavirus, especially novel coronavirus, and has the potential of being developed into a medicine for treating and preventing the coronavirus, especially resisting the novel coronavirus.

Description

technical field [0001] The present invention relates to the technical field of a class of medicinal chemistry, in particular to the use of Vilanterol or a pharmaceutically acceptable salt thereof in the preparation of anti-coronavirus inflammatory drugs, and in more detail Vilanterol may be used as an effective papain-like protease PLPro for coronavirus. inhibitor. Background technique [0002] Coronaviruses belong to the order Nesteviridae, the family Coronaviridae, and the genus Coronaviridae. They are a large class of viruses that widely exist in nature, and have the largest genome among the currently known positive-strand RNA viruses. At the same time, coronavirus is a type of RNA virus with an envelope and a single-segment positive-strand RNA virus. In short, the genome of the coronavirus is composed of only one RNA chain, and the genetic information is carried by RNA. When the virus enters the host cell Afterwards, the host's ribosomes can be used directly to produce ...

Claims

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Application Information

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IPC IPC(8): A61K31/137A61P31/14
CPCA61K31/137A61P31/14
Inventor 韩克利贾燕王艺颖
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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