Application of halogenated furanone compounds to preparation of HIV-1 (Human Immunodeficiency Virus-1)-resistant drugs

A HIV-1, halogenated furan technology, applied in the field of application of halogenated furan compounds in the preparation of anti-HIV-1 virus drugs, can solve the problems of anti-virus experiments of compounds that have not been reported

Inactive Publication Date: 2014-08-27
SUN YAT SEN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] X is a halogen; R is an alkane group of C1~C4; n is an integer of 1~4, such as (2-[(5-Bromofuran-2-yl)carboxamido]-N-(3-methylbutyl)acetamide, 5-bromo-N-(2-(isopentylamino)-2-oxoethyl)furan -2-carboxamide) can be purchased from Enamine Company or 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

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  • Application of halogenated furanone compounds to preparation of HIV-1 (Human Immunodeficiency Virus-1)-resistant drugs
  • Application of halogenated furanone compounds to preparation of HIV-1 (Human Immunodeficiency Virus-1)-resistant drugs
  • Application of halogenated furanone compounds to preparation of HIV-1 (Human Immunodeficiency Virus-1)-resistant drugs

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Embodiment Construction

[0021] 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.

[0022] 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 an application of halogenated furanone compounds to preparation of HIV-1 (Human Immunodeficiency Virus-1)-resistant drugs. The compounds have the general formula as shown in the specification, wherein X is a halogen; R is one of C1-C4 alkyls; and n is an integer selected from 1-4. Based on the interaction of Vif-APOBEC3G, the inventor proves that the expression quantity of green fluorescent proteins in a screening system is to be recovered because the compounds as shown in the general formula and particularly 2-[(5-brominated furan-2-yl)carbamyl]-N-(3-methylbutyl)acetamide can inhibit the degrading activity of Vif proteins to A3G. Wild HIV-1 infection experiments carried out in human primary CD4+T lymphocytes and CD4+T lymphocytic systems such as H9, SupT1 and the like prove that 2-[(5-brominated furan-2-yl)carbamyl]-N-(3-methylbutyl)acetamide has a relatively good antiviral effect. The halogenated furanone compounds are used for providing powerful theoretical and practice basis for further researching and developing antiviral drugs so as to have important research and development values and development significance.

Description

technical field [0001] The invention relates to a new application of a compound, in particular to the application of halogenated furan 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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/341A61P31/18
Inventor 张辉潘婷罗海华张旭何欣
Owner SUN YAT SEN UNIV
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