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Application of derivative of polysubstituted acyl thiourea pyrimidine for preparing antiviral medicine

A kind of technology of acylthiouracil and antiviral drug, which is applied in the field of chemical synthesis of active compounds

Inactive Publication Date: 2007-01-31
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, acylthiourea compounds are currently only used as herbicides

Method used

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  • Application of derivative of polysubstituted acyl thiourea pyrimidine for preparing antiviral medicine
  • Application of derivative of polysubstituted acyl thiourea pyrimidine for preparing antiviral medicine
  • Application of derivative of polysubstituted acyl thiourea pyrimidine for preparing antiviral medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Using the above method, the following compounds were tested for their antiviral activity against hepatitis B virus, influenza virus and herpes virus. Table 1 and Table 2 are the results of the determination of the antiviral activity of the following compounds on hepatitis B virus, influenza virus and herpes virus.

[0034]

[0035] Numbering

[0036] Among them, "+" means active, "-" means inactive

[0037] compound

[0038] "+" means active, "-" means inactive

Embodiment 2

[0040] Using the above method, the following compounds were tested for their antiviral activity against hepatitis B virus, influenza virus and herpes virus. Table 3 and Table 4 are the results of the determination of the antiviral activity of the following compounds on hepatitis B virus, influenza virus and herpes virus.

[0041]

[0042] Numbering

R1

R2

R3

X

Y

anti flu

activity

Anti-hepatitis B

HBsAG

HBeAG

Anti-herpes

activity

10

H

CL

H

Oh

CH 3

+

+ +

+

11

H

CL

H

OCH 3

OCH 3

+

+ +

+

12

F

F

H

Oh

CH 3

-

- -

+

13

Cl

Cl

H

OC 2 h 5

OC 2 h 5

+

+ +

+

14

H

Cl

H

Cl

Cl

+

+ +

+ ...

Embodiment 3

[0046] Using the above method, the following compound N'-(4,6-diethoxypyrimidin-2-yl)-N-3-methyl-2-(4-chlorophenyl)butyrylthiourea was tested for influenza virus and herpesvirus antiviral activity assays. Table 5 is the results of the determination of the antiviral activity of the compounds against influenza virus and herpes virus (unit: μM).

[0047]

[0048] TD 50

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PUM

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Abstract

An application of polysubstituent acylthiouracil derivative in preparing the antiviral diseases, such as influenza and herpes, is disclosed.

Description

technical field [0001] The invention belongs to the field of chemically synthesizing active compounds, and in particular relates to the use of multi-substituted acylthiouracil derivatives in the preparation of antiviral drugs. Background of the invention: [0002] Since Beijerinck first proposed the concept of viruses in 1898, the types of viruses have grown from dozens to more than 4,000 today. Especially in recent years, HIV virus, hepatitis B virus, SARS virus and avian influenza virus have caused extremely serious harm to public health all over the world, and have once again aroused the general attention of global antiviral drug research. However, the research progress of antiviral drugs is slow. So far, more than 30 kinds of drugs have been developed, among which there are no real specific drugs for HIV virus, hepatitis B virus, SARS virus and avian influenza virus. The situation is extremely grim. Pyrimidine compounds widely exist in organisms, and three of the five m...

Claims

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Application Information

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IPC IPC(8): A61K31/505A61P1/16A61P31/14A61P31/16A61P31/22
Inventor 周珮冯美卿孙传文黄海周伟
Owner FUDAN UNIV
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