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Application of benzothiadiazole compound in preparation of medicine for resisting SARS-COV-2 novel coronavirus

A technology of SARS-COV-2 and benzothiadiazoles, applied in the field of medicine

Active Publication Date: 2022-03-11
JIANGNAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, there is a lack of effective anti-SARS-COV-2 novel coronavirus drugs

Method used

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  • Application of benzothiadiazole compound in preparation of medicine for resisting SARS-COV-2 novel coronavirus
  • Application of benzothiadiazole compound in preparation of medicine for resisting SARS-COV-2 novel coronavirus
  • Application of benzothiadiazole compound in preparation of medicine for resisting SARS-COV-2 novel coronavirus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Preparation of a benzothothiane compound

[0031]

[0032] Reagents and conditions: a) Dichloride, toluene; B) iron powder, ammonium chloride, ethanol, water; c) benzaldehyde, sodium borohydride, methanol.

[0033] Compound 15 (2 g, 13.07 mmol) of toluene (20 mL) was placed in three flasks (100 mL), and DMF (0.1 mL) and SOCL were sequentially added under ice bath. 2 (3.76 mL, 52.28 mmol), after the dropwise addition, the reaction solution was transferred into a 65 ° C oil bath, and the reaction was stirred for 3 h. After the monitoring reaction was complete, the filtrate was concentrated to give a purified compound 16 (2.2 g, yield 93.2%).

[0034] The compound 16 (2 g, 11.04 mmol) and NH 4 CL (2.34 g, 44.20 mmol) of ethanol and water (2: 1,3 ml) solution was placed in a 90 ° C oil bath for 30 min and then add iron powder (2.47 g, 44.20 mmol), and continued reflux and stirring reaction for 3h, monitoring After the reaction is complete, heat filtration, filter re...

Embodiment 2

[0059] Example 2 Benzothiane compound detection of SARS-COV-2 3ClPro protease activity:

[0060] Based on SARS-COV-2 3ClPro protein is the basic characteristics of proteolytic enzymes, and the screening system of SARS-COV-2 3ClPro protein activity is established by establishing fluorescence. SARS-COV-2 3Clpro protein specifically shear P1 bits of Gln (q) substrate, the activity detection can be used as a substrate to reflect the activity of the proteolytic enzyme by detecting the generation of fluorescent signals. SARS-COV-2 3ClPro protease activity Test uses fluorescent labeled polypeptide substrates (sequence: MCA-AVLQSGFRK (DNP) K), SARS-COV-2 3ClProase solution (diluted in the reaction liquid to 0.5 μm) and compound in reaction liquid (20 mm Tris, pH 7.3, 150 mM NaCl, 1 mM EDTA, 1% Glycerol, 0.01% Tween-20) was incubated for 10 minutes, and the substrate (40 μm, 50 μl of reaction liquid) was added, and the reaction was started after the reaction was used after Envision Multila...

Embodiment 3

[0062] Example 3 Benzothothiadiazole compounds for SARS-COV-2PLPRO protease activity inhibitory effect:

[0063] Based on SARS-COV-2PLPRO protein is the basic characteristics of proteolytic enzymes, and the screening system of SARS-COV-2PLPRO protein activity is established. SARS-COV-2 PLPRO protein can specifically identify and cut the bisglycine polypeptide, and the active detection can use a fluorescent polypeptide to react to the activity of its protein hydrolase by detecting the formation of fluorescent signals. SARS-COV-2PLPRO protease activity Test uses coumarin labeled polypeptide substrate (sequence: Z-RLRGG-AMC), SARS-COV-2PLPRO enzyme solution (diluted in the reaction liquid to 40 nm) and compound in reaction liquid (20 mm TRIS pH 8.0, 0.01% Tween 20, 0.5 mm DTT) The medium temperature was incubated for 10 minutes, and the substrate (50 μm, total volume of reaction liquid) was added, and the fluorescence intensity of the reaction liquid was detected using EnVision Multi...

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Abstract

The invention discloses application of a benzothiadiazole compound in preparation of a medicine for resisting SARS-COV-2 novel coronavirus, and belongs to the technical field of medicine. According to the present invention, the micro-mole-level benzothiadiazole compound having the structure represented by the general formula (I) is utilized to provide inhibition activity for two types of proteins, such that the anti-SARS-CoV-2 Wuhan strain virus activity is provided; according to the present invention, the benzothiadiazole compound is firstly provided to be adopted as the SARS-COV-2 novel coronavirus inhibitor, such that the new thought and the new use are provided for prevention and / or treatment of the SARS-COV-2 novel coronavirus, and the important medical research value is provided.

Description

Technical field [0001] The present invention belongs to the field of medical technology, and more particularly to the application of a benzothothiadazole compound in the preparation of anti-SARS-COV-2 new coronaviral drugs. Background technique [0002] New coronavirus pneumonia (COVID-19) is a serious threat to human health in human health due to severe acute respiratory syndrome (SARS-COV-2). SARS-COV-2 is a RNA virus containing the envelope, composed of an outer film and an inner layer of core mill. The envelope is the same as the cell membrane as a phospholipid dual molecular layer structure, including a viral genome encoded structural protein, including spike glycoprotein, S protein, envelope protein (E protein) and membrane protein (MEMBRANEPROTEIN, M protein). The nucleus shell is assembled from NucleocapsidProtein, N protein and virus RNA. In the nucleic acid and protein synthesis stage, 2 function open reading frames of coronaviruses, translated multimerin 1a (polyprotei...

Claims

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Application Information

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IPC IPC(8): A61K31/433A61P31/14A61P11/00
CPCA61K31/433A61P31/14A61P11/00Y02A50/30
Inventor 王文龙李佳冯勃臧奕闫薛
Owner JIANGNAN UNIV
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