Application of cyano-pyrridine compounds to prepare anti-HIV-1 medicines

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

Inactive Publication Date: 2014-09-03
SUN YAT SEN UNIV
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  • Description
  • Claims
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Problems solved by technology

[0007] X is S or O, such as (ethyl 5-cyanide Base-6-thioxylidene-1,6-dihydropyridine-2-carboxylate, ethyl 5-cyano-6-thioxo-1,6-dihydropyridine-2-carboxylate) can be purchased from Enamine Company or on its basis Artificially synthesized on the Internet, there is no report that this type of compound is used in antiviral experiments or other similar effects

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  • Application of cyano-pyrridine compounds to prepare anti-HIV-1 medicines
  • Application of cyano-pyrridine compounds to prepare anti-HIV-1 medicines
  • Application of cyano-pyrridine compounds to prepare anti-HIV-1 medicines

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Embodiment Construction

[0023] 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 HIV-1 virus. It exists in HIV-1 natural host cells (such as CD4+ T cells and macrophages), can be packaged into HIV-1 virus particles, and is reverse transcribed in HIV-1 In the process, it exerts its strong antiviral effect. For this reason, HIV-1 itself encodes the Vif protein to specifically resist the antiviral activity of APOBEC3G, which can import 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.

[0024] According to the molecular mechanism of Vif antagonizing APOBEC3G, several small molecule drugs that can prevent HIV Vif from degrading APOBEC3G were screened out. To this end, we will establish a simple living cell screening system, such as figure 1 As shown in B, plasmids ex...

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Abstract

The invention discloses application of cyano-pyrridine compounds to prepare anti-HIV-1 medicines. The general formula of the compounds is shown in the specification. In the general formula, R is H or a C1-C4 alkane, and X is S or O. By utilizing the interaction of Vif-APOBEC3G, the compounds with the above general formula, especially ethyl 5-cyano-6-thioxo-1,6-dihydropyridine-2-carboxylate is confirmed to be capable of inhibiting the activity of Vif protein on degrading A3G and leading rising up of expression level of green fluorescent protein in a screening system. By performing wild-type HIV-1 infection experiments on human primary CD4+T lymphocyte and H9, SupT1 and other CD4+T lymphocytic series, ethyl 5-cyano-6-thioxo-1,6-dihydropyridine-2-carboxylate is further confirmed to have relatively good antiviral effect. A powerful theoretical basis and a practice basis are provided for further research and development of antiviral medicines, and the compounds have important value on research and development and exploitation meaning.

Description

technical field [0001] The invention relates to a new application of a compound, in particular to the application of cyano-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 a per...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/44A61P31/18
Inventor 张辉潘婷罗海华张旭何欣
Owner SUN YAT SEN UNIV
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