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Novel iodine-containing antiviral drug

An antiviral drug and virus technology, applied in antiviral agents, active ingredients of iodine compounds, pharmaceutical formulations, etc., can solve the problem that the cccDNA library in the nucleus is not affected, and achieve good physiological activity and reduce activity.

Active Publication Date: 2021-01-29
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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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] This 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] Iodo groups used to damage the genetic material of viruses.

[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 a stable isotope of iodine 127 I.

[0036] Carry out cell experiments with the above-mentioned iodine-containing antiviral drugs, and do anti-hepatitis B virus activity test; the results compared with other drugs are as follows:

[0037] 1. The effect of iodine-containing antiviral drugs and entecavir on inhibiting the expression of cccDNA of hepatitis B virus is as follows: image 3 Shown: cccDNA expression levels were measured 48h and 72h after the addition of iodine-containing antiviral drugs and entecavir. ...

Embodiment 2

[0042] The difference between this embodiment and Embodiment 1 is that the iodine element in the iodo group is a radioactive isotope of iodine 125 I.

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Abstract

The invention provides a novel iodine-containing antiviral drug, the chemical structural general formula of which is shown as formula 1, and comprises a bonding group for binding viral genetic materials; and iodo groups for destroying viral genetic material. The compound has good physiological activity and is expected to become a novel anti-hepatitis B virus drug.

Description

technical field [0001] The invention relates to a novel iodine-containing antiviral drug. Background technique [0002] Viral hepatitis B (referred to as hepatitis B) is an infectious disease caused by hepatitis B virus (Hepatitis B Virus, HBV) infection, with the liver as the target organ, and the cellular immunopathological changes leading to its functional damage, which can develop into a chronic disease. Liver disease, liver cirrhosis, and liver cancer are important public health problems worldwide. my country is a high-incidence area of ​​hepatitis B. According to the results of the second serological epidemiological survey of HBV infection in my country, there are about 120 million HBV carriers in the country, and the HBV infection rate accounts for about 3.2% of the total population. The total number is about 42 million, and most of them are chronic. persistent infection. [0003] Covalently closed circular DNA (cccDNA) is an important cause of chronic hepatitis B pe...

Claims

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Application Information

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Patent Type & Authority Applications(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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