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Application of MK-0893 in preparation of products for inhibiting coronavirus and medicines for resisting coronavirus infection

A kind of MK-0893, 1. The technology of MK-0893, applied in the application fields of products and anti-coronavirus infection drugs

Pending Publication Date: 2022-05-17
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After reviewing relevant information, no relevant reports were found that the compound MK-0893 can inhibit the activity of coronavirus papain-like protease (PLPro)

Method used

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  • Application of MK-0893 in preparation of products for inhibiting coronavirus and medicines for resisting coronavirus infection
  • Application of MK-0893 in preparation of products for inhibiting coronavirus and medicines for resisting coronavirus infection
  • Application of MK-0893 in preparation of products for inhibiting coronavirus and medicines for resisting coronavirus infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Under the action of different concentrations of MK-0893, the fluorescence intensity of the substrate peptide under the metabolism of papain-like protease changes with time

[0036] The specific implementation process is:

[0037] (1) The stock solutions of SARS-CoV-2 papain-like protease and substrate peptide were stored in a -80°C refrigerator;

[0038] (2) Thaw SARS-CoV-2 papain-like protease in a freezing plate (-4 to 4°C) at room temperature, take 1uL and dilute it in 98uL borate borax buffer (PH=7.4), and add it to the detection plate;

[0039] (3) Add 1uL of different concentrations of MK-0893 at 0, 0.05mM, 0.5mM, 1mM, and 2.5mM to the solution obtained in the above step (2);

[0040] (4) Add 1uL of the same concentration of substrate peptide (0.5mM) to the solution obtained in the above step (3), incubate at 37°C with a fluorescent microplate reader, and use a fluorescent microplate reader to monitor excitation at 342nm and fluorescence emission at 49...

Embodiment 2

[0043] Example 2: Inhibitory ability of compound MK-0893 to novel coronavirus papain-like protease

[0044] The specific implementation process is as follows:

[0045] (1) The stock solutions of SARS-CoV-2 papain-like protease and substrate peptide were stored in a -80°C refrigerator;

[0046] (2) Thaw SARS-CoV-2 papain-like protease in a freezing plate (-4 to 4°C) at room temperature, take 1uL and dilute it in 98uL borate borax buffer (PH=7.4), and add it to the detection plate;

[0047] (3) Add 1uL of different concentrations of MK-0893 at 0, 0.05mM, 0.5mM, 1mM, and 2.5mM to the solution obtained in the above step (2);

[0048] (4) Add 1uL of the same concentration of substrate peptide (0.5mM) to the solution obtained in the above step (3), incubate at 37°C with a fluorescent microplate reader, and use a fluorescent microplate reader to monitor excitation at 342nm and fluorescence emission at 496nm Value, detect while incubating, incubate for 1h;

[0049] (5) The fluoresc...

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Abstract

The invention relates to application of MK-0893 in preparation of products for inhibiting coronavirus and medicines for resisting coronavirus infection. The invention also provides a coronavirus papaya-like protease inhibitor, and the inhibitor is MK-0893 or an optical isomer thereof, a hydrate thereof and a pharmaceutically acceptable salt thereof. The invention provides application of MK-0893 serving as a coronavirus papaya-like protease (PLPro) inhibitor to preparation of products for inhibiting coronavirus and preparation of medicines for resisting coronavirus infection by utilizing a relatively strong inhibition effect of MK-0893 on the enzymatic activity of target papaya-like protease (PLPro) of the coronavirus, and particularly provides application of MK-0893 serving as the coronavirus papaya-like protease (PLPro) inhibitor to preparation of products for inhibiting the coronavirus and preparation of medicines for resisting coronavirus infection. A new thought is provided for treating and preventing coronavirus infection, especially resisting new coronavirus infection.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to the application of MK-0893 in the preparation of coronavirus-inhibiting products and anti-coronavirus infection drugs. Background technique [0002] Coronavirus is an enveloped virus with a positive-strand RNA genome, that is, a methylated "cap" at the 5' end of the RNA strand, a PolyA "tail" structure at the 3' end, and a helically symmetrical nucleocapsid protein. The genome size is At 27 to 32 kb, the genome is the largest among known positive-strand RNA viruses. Under the electron microscope, coronavirus particles are irregular in shape, with a diameter of about 60-220nm and an average diameter of 100nm. called coronavirus. [0003] According to the host, serotype gene sequence and structure, coronaviruses can be divided into four categories: α, β, γ and δ. Among these four types, α and β can only infect mammals, and γ and δ mainly infect birds; α coronaviruses...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/415A61P31/14
CPCA61K31/415A61P31/14
Inventor 韩克利王艺颖贾燕张洪苓
Owner SHANDONG UNIV