A novel iodine-containing antiviral drug

An antiviral drug, a technology of chemical structural formula, applied in the direction of antiviral agents, active ingredients of iodine compounds, pharmaceutical formulations, etc., can solve the problem of no effect on the nuclear cccDNA library, and achieve the effect of good physiological activity and reduced activity

Active Publication Date: 2022-08-05
THE THIRD AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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  • Abstract
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AI Technical Summary

Problems solved by technology

[0007] The defect of the above-mentioned technical scheme is: the existing clinical anti-HBV drugs have no effect on the cccDNA pool in the nucleus

Method used

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  • A novel iodine-containing antiviral drug
  • A novel iodine-containing antiviral drug
  • A novel iodine-containing antiviral drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The present embodiment provides a novel iodine-containing antiviral drug, the general chemical structure of which is shown in formula 1, including:

[0032] Bonding groups for binding viral genetic material;

[0033] The iodine group used to destroy viral genetic material.

[0034] Among them, the bonding group includes two hydroxyl groups, which can be combined with a phosphorus atom to form a phosphodiester bond.

[0035] The iodine element in the iodo group is the stable isotope of iodine 127 I.

[0036] Cell experiments were performed with the above-mentioned iodine-containing antiviral drugs, and anti-HBV activity tests were performed; the results compared with other drugs are as follows:

[0037] 1. Comparison of the effects of iodine-containing antiviral drugs and entecavir in inhibiting the expression of HBV cccDNA image 3 Shown: cccDNA expression was measured at 48h and 72h after adding iodine-containing antiviral drugs and entecavir, respectively. The res...

Embodiment 2

[0042] The difference between this example and Example 1 is that the iodine element in the iodo group is a radioisotope of iodine 125 I.

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Abstract

The present invention provides a novel iodine-containing antiviral drug, the general chemical structure of which is shown in formula 1, including: a bond-forming group for binding viral genetic material; and an iodine group for destroying viral genetic material. The invention has better physiological activity and is expected to become a new type of anti-hepatitis B virus drug.

Description

technical field [0001] The invention relates to a novel iodine-containing antiviral drug. Background technique [0002] Hepatitis B (hepatitis B for short) is an infectious disease caused by hepatitis B virus (Hepatitis B Virus, HBV) infection. Liver disease, liver cirrhosis, and liver cancer are an important public health problem worldwide. my country is a high incidence area of ​​hepatitis B. The results of the second HBV infection seroepidemiological survey in my country show that there are about 120 million HBV carriers in the country, and the HBV infection rate accounts for about 3.2% of the total population, with a total of about 42 million, most of whom are chronic. persistent infection. [0003] Covalently closed circular DNA (cccDNA) is an important cause of persistent chronic hepatitis B infection and the main cause of relapse after antiviral therapy. The cellular immune response triggered by it can not only cause liver parenchyma damage, but also lead to Chronic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519A61K33/18A61P31/20
CPCA61K31/519A61K33/18A61P31/20
Inventor 谢良骏
Owner THE THIRD AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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