Application of Naphthalene-Pyridine Compounds in the Preparation of Anti-HIV-1 Virus Drugs

A technology of HIV-1 and pyridines, which is applied in the new application field of compounds, can solve the problems of anti-virus experiments of compounds that have not been reported

Active Publication Date: 2016-02-17
SUN YAT SEN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] R, R 1 Independently H, methyl or ethyl, respectively located at the 1'~4' position or the 5~8 position, such as (1-(naphthalen-1-ylmethyl)-1,2-dihydropyridin-2-one, 1-(naphthalen-1-ylmethyl)pyridin-2(1H)-one) can be purchased from Enamine or in It is artificially synthesized on the basis of it, and there is no report that this type of compound is used in antiviral experiments or other similar effects

Method used

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  • Application of Naphthalene-Pyridine Compounds in the Preparation of Anti-HIV-1 Virus Drugs
  • Application of Naphthalene-Pyridine Compounds in the Preparation of Anti-HIV-1 Virus Drugs
  • Application of Naphthalene-Pyridine Compounds in the Preparation of Anti-HIV-1 Virus Drugs

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Embodiment Construction

[0022] Vif is one of the essential proteins of HIV, and its main function is to antagonize the natural antiviral factor APOBEC3G in the host. APOBEC3G is a major threat to the HIV-1 virus. It exists in the natural host cells of HIV-1 (such as CD4+T cells and macrophages) and can be packaged into HIV-1 virus particles. Play its extremely strong antiviral effect in the process. For this reason, HIV-1 itself encodes the Vif protein to specifically combat the antiviral activity of APOBEC3G, which can introduce APOBEC3G into the ubiquitin system and degrade it ( figure 1 A). Therefore, how to inactivate Vif is a very important target for the development of anti-HIV-1 virus drugs.

[0023] According to the molecular mechanism of Vif antagonizing APOBEC3G, several small molecule drugs that can prevent HIV Vif from degrading APOBEC3G have been screened out. To this end, we will establish a simple living cell screening system, such as figure 1 As shown in B, a plasmid expressing APOBEC3...

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Abstract

The invention discloses the application of naphthalene-pyridine compounds in the preparation of anti-HIV-1 virus drugs. The general formula of the compound is? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? In the formula: the group is located at position 1 or 2; R and R1 are independently H, methyl or ethyl, and are located at positions 1'-4' or positions 5-8 respectively. The inventors used the interaction of Vif-APOBEC3G to confirm that the compound of the above general formula, especially 1-(naphthalene-1-ylmethyl)-1,2-dihydropyridin-2-one can inhibit the activity of Vif protein from degrading A3G , resulting in a rise in the expression of green fluorescent protein in the screening system. By primary CD4+ in humans? T lymphocytes and H9, SupT? 1 etc. CD4+? Infection experiment of wild type HIV-1 virus in T lymphocyte line further confirms that it has better antiviral effect. It provides a strong theoretical basis and practical basis for further research and development of antiviral drugs, and has important research and development value and significance.

Description

technical field [0001] The invention relates to a new application of a compound, in particular to the application of naphthalene-pyridine compounds in the preparation of anti-HIV-1 virus drugs. Background technique [0002] The HIV-1 virus was first discovered in the United States in 1981. After a series of unexplained syndromes characterized by cellular immune deficiency appeared, researchers began to search for its pathogenic source. In 1983, a French research team isolated the HIV-1 virus from the lymph nodes of a patient with lymphoma syndrome. It is a lentivirus that infects the cells of the human immune system, which destroys the body's immunity and causes the immune system to lose its resistance, causing various diseases and cancers to survive in the human body, resulting in Acquired Immunodeficiency Syndrome— -AIDS. At present, due to insufficient popularization of AIDS education, the global HIV infection is still on the rise, especially in China, which has entered...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4402A61P31/18
Inventor 张辉潘婷罗海华张旭何欣
Owner SUN YAT SEN UNIV
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