Application of benzene-sulfamide compounds in preparing anti-HIV-1(human immunodeficiency virus-1) drug

A technology of HIV-1 and sulfonamides, applied in antiviral agents, active ingredients of heterocyclic compounds, pharmaceutical formulations, etc., can solve problems such as antiviral experiments of unreported compounds

Active Publication Date: 2014-07-02
SUN YAT SEN UNIV
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0008] It can be purchased from Enamine Company or artificially synthesized on the basis of it. Currently, there is no report that this type of compound is used in antiviral experiments or other possible effects

Method used

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  • Application of benzene-sulfamide compounds in preparing anti-HIV-1(human immunodeficiency virus-1) drug
  • Application of benzene-sulfamide compounds in preparing anti-HIV-1(human immunodeficiency virus-1) drug
  • Application of benzene-sulfamide compounds in preparing anti-HIV-1(human immunodeficiency virus-1) drug

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Embodiment Construction

[0028] RRE (Rev-responding element) is a special RNA structure in HIV, which consists of five rod-loop structures and can bind to the regulatory protein Rev. Rev is one of the two regulatory genes unique to HIV, encoded by two exons through splicing. The protein synthesized by Rev consists of 116 amino acids with a molecular weight of about 19kD. It is a basic and phosphorylated protein. Polymers can be formed both in vitro and in cells, and amino acids 18-60 are involved in the formation of multimers. Between R35 and R51, there are many basic amino acids, these amino acids are the sites of Rev assembly RRE RNA, and 40NRRRW45 also plays the role of nuclear import signal. The leucine-rich group plays a key role for Rev to complete its transfer RNA function.

[0029] There are SD and SA cleavage sites on PDM628. When the Rev protein does not exist, the luciferase gene carried on PDM 628 is clipped, resulting in a small amount of luciferase expression; when the two plasmids are...

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Abstract

The invention discloses an application of benzene-sulfamide compounds in preparing an anti-HIV-1(human immunodeficiency virus-1) drug. A general formula of the benzene-sulfamide compounds is as shown in the specification, wherein X1-X4 are independently selected from halogen, H and -NO2, and have one -NO2 at the same time at most; X1-X4 are not halogen at the same time; R1 is selected from the substances as shown in the specification, wherein Y is C or N, n is an integer of 2-6, R3 is H or a statured chain hydrocarbon or a cyclic hydrocarbon with carbon number not exceeding 5, R4 is H or saturated chain hydrocarbons of C1-C4; R2 is selected from H, halogen or substance as shown in the specification; Y1 and Y2 are independently selected from H, halogen, and methyl. By applying the binding characteristic of Rev-RRE (response element), the inventor proves that the benzene-sulfamide compounds with the general formula can restrain Rev protein activity, causes expression quantity of luciferase in a screening system to reduce, and has a good antiviral effect. Moreover, powerful theoretical basis and practice basis are provided for further developing the antiviral drug, and therefore, the application has important development value and development significance.

Description

technical field [0001] The invention relates to a new application of a compound, in particular to the application of benzene-sulfonamide 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 Applications(China)
IPC IPC(8): A61K31/4706A61K31/4184A61K31/50A61P31/18
Inventor 张辉潘婷罗海华张旭柏川
Owner SUN YAT SEN UNIV
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