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Application of benzimidazole compound in preparation of anti-hepatitis B virus drugs

A technology of hepatitis B virus and benzimidazole, which is applied in the field of medicine, can solve the problems of drug resistance, inability to clear the virus, poor tolerance of patients, etc., achieve high effectiveness and safety, inhibit replication, and broad application prospects Effect

Pending Publication Date: 2022-01-21
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although nucleoside (acid) analogues show a strong virus suppression effect in most patients with hepatitis B, they cannot clear the infected virus, must be taken continuously, and are prone to drug resistance
Interferon therapy has many side effects and is poorly tolerated by patients. Therefore, only a small number of patients are suitable for interferon therapy

Method used

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  • Application of benzimidazole compound in preparation of anti-hepatitis B virus drugs
  • Application of benzimidazole compound in preparation of anti-hepatitis B virus drugs
  • Application of benzimidazole compound in preparation of anti-hepatitis B virus drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Compounds inhibit the formation of HBV capsids

[0030] In this embodiment, the inhibitory effect of different concentrations of compounds on HBV capsid formation in cells is observed through capsid detection experiments and Western Blot experiments. The specific process is:

[0031] 1. Inoculate Huh7 cells (the Huh7 cells are provided by the Chinese Academy of Sciences Cell Bank / Stem Cell Bank) suspension (2 × 10 cells) in a 24-well plate 5 cells / well), the culture plate was pre-cultured in the incubator for 12 hours, and the cells adhered to the wall.

[0032] 2. Use 2 μl of Turbofect transfection reagent (Thermo Fisher Scientific, Waltham, USA) and 1 μg pCDN3 / Core plasmid or p1.3×HBV plasmid in each well for transfection experiments, and add different concentrations of The compound of formula (I) was reacted for 48 hours, and samples were collected and extracted. The pCDN3 / Core plasmid in this step was obtained by construction. The specific method was: c...

Embodiment 2

[0044] Example 2: Effects of compounds on the assembly of Cp149 protein to form a capsid

[0045] In this example, the impact of the compound on the assembly of the Cp149 protein to form a capsid was observed through a transmission electron microscope. The specific process is:

[0046] 1. Mix the prokaryotically expressed Cp149 protein (1mg / ml) with a solution containing 150mM Hepes and 15mM NaCl at a ratio of 1:2, add 10μM compound of formula (I), and act at 37°C for 1h.

[0047] 2. Negative staining: Use a pipette gun to draw 20 μl of sample and drop it on a 150-mesh carbon-coated copper grid for 3-5 minutes, then use filter paper to absorb excess liquid. Drop 2% phosphotungstic acid on the carbon support film copper mesh and place it for 1-2min, absorb excess liquid with filter paper, and dry at room temperature.

[0048] 3. Observe under a transmission electron microscope, and collect images for analysis. The result is as figure 2 shown.

[0049] figure 2 The result...

Embodiment 3

[0050] Example 3: Inhibitory Effect of Compounds on HBV Replication

[0051] This embodiment observes the inhibitory effect of different concentrations of compounds on HBV replication by Southern blot, the specific process is:

[0052] 1. Inoculate HepAD38 and Huh7 cell suspensions (1×10 6 cells / dish), the culture dish was pre-cultured in the incubator for 12 hours, and the cells adhered to the wall. HepAD38 is a cell line that sustainably expresses and produces HBV constructed on the basis of the HepG2 cell line (references: Ladner, S.K.; Otto, M.J.; Barker, C.S.; etc., Inducible expression of human hepatitis B virus (HBV) in stably transfected hepatoblastoma cells : a novel system for screening potential inhibitors of HBV replication. Antimicrob Agents Chemother 1997,41,(8),1715-20). Different concentrations of the compound of formula (I) were added to the HepAD38 cell culture dish, and the samples were collected after acting for 48 hours.

[0053] 2. Each plate of Huh7 c...

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Abstract

The invention discloses an application of a benzimidazole compound in preparation of anti-hepatitis B virus drugs. The benzimidazole compound is a novel nucleocapsid inhibitor, and can effectively inhibit assembly of hepatitis B virus core protein and replication of hepatitis B virus. The benzimidazole compound provided by the invention has a wide application prospect in the preparation of anti-HBV drugs and drugs for treating hepatitis B virus infection related diseases, solves the problem that effective anti-HBV drugs are urgently needed at present, and provides a new application of the benzimidazole compound in the anti-HBV drugs.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of a benzimidazole compound in the preparation of anti-hepatitis B virus drugs. Background technique [0002] Hepatitis B virus (HBV) is a hepadnavirus that infects humans mainly through blood and mother-to-child routes. There are at least 257 million people with chronic HBV infection worldwide, and chronic HBV infection can cause diseases such as chronic hepatitis, liver cirrhosis, and hepatocellular carcinoma. About 1 million people die each year from liver disease associated with HBV infection. Therefore, the treatment of HBV chronic infection is one of the important tasks related to public health. [0003] At present, nucleoside (acid) analogs (such as entecavir, tenofovir) and interferon drugs are mainly used in the treatment of chronic HBV infection. Although nucleoside (acid) analogues show a strong virus suppression effect in most patients with hepat...

Claims

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Application Information

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IPC IPC(8): A61K31/4184A61P31/20A61P1/16
CPCA61K31/4184A61P31/20A61P1/16
Inventor 谢幼华王鑫宋迎迎唐宇李俪刘晶
Owner FUDAN UNIV
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