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Application of benzamide derivative to preparing drug for treating AIDS (Acquired Immune Deficiency Syndrome)

A benzamide and anti-AIDS technology, applied in the field of biomedicine, can solve problems such as poor curative effect

Inactive Publication Date: 2010-12-22
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The progress made in the research and clinical application of anti-HIV infection drugs is of great significance to the control and treatment of AIDS, but even if the most effective treatment plan is used, the treatment only accounts for 20% to 50% of the number of people treated, and the curative effect is not good

Method used

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  • Application of benzamide derivative to preparing drug for treating AIDS (Acquired Immune Deficiency Syndrome)

Examples

Experimental program
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Effect test

Embodiment 1

[0043] Embodiment 1 compound anti-HIV-1 virus increment test

[0044] MT-2 cells were planted in a 96-well plate, 10 per well 4 indivual. The medium is RPMI 1640 medium containing 10% fetal bovine serum. HIV-1 virus was used to infect the cells with 100 50% tissue infection equivalents, and at the same time, the compound was added with different concentration gradients and cultured overnight (the well without compound was used as the blank control). The next day, replace with fresh medium without small molecule compounds. On the fourth day, get 100uL of the culture supernatant, add 5% volume of Triton-X100 to obtain the virus lysate, and then use the ELISA method to measure the p24 protein content (p24 is the coat protein of HIV-1, which can be used as a measure of the number of virions) index of). Simply put, the double-antibody sandwich method is used to measure the amount of p24 protein produced in each well. Coat the plate with anti-HIV immunoglobulin overnight (pH 9....

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Abstract

The invention belongs to the biomedicine field and relates to application of a small molecular compound with anti-HIV (Human Immunodeficiency Virus) activity to preparing a drug for treating AIDS (Acquired Immune Deficiency Syndrome). The AIDS called as a contemeporary plague and a super cancer draws great attentions of World Health Organization (WHO) and national governments, however, an effective drug for treating the disease does not exist so far. The invention provides application of N-(3-(benzamide)-5-(4-oxo-4H-3,1-benzoxazine-2-yl) phenyl) benzamide to preparing the drug for treating the AIDS. The compound has the ability of inhibiting HIV-1 virus replication, is a drug designed aiming to a cell target, is not easy to cause the drug resistance and is suitable for the needs of lifelong medication of an AIDS patient.

Description

technical field [0001] The invention relates to the field of biomedicine, and relates to the application of a small molecular compound with anti-HIV activity in the preparation of anti-AIDS drugs. Background technique [0002] Human immunodeficiency virus (HIV) is a special class of retroviruses. It has a high degree of variability, can specifically infect and kill the main immune cell population, and can induce enhanced antibodies. In recent years, due to the better understanding of the pathogenesis of HIV infection, new and more effective drugs have been developed, such as protease inhibitors (pi) and non-nucleoside reverse transcriptase inhibitors (nnrti). The mechanism of action and application of commonly used anti-HIV drugs are briefly described as follows. [0003] 1. Protease Inhibitors [0004] Mechanism of action of protease inhibitor pi: Proteases are essential for gag, gagpol polyproteins and post-translational processing, structural proteins that form the cor...

Claims

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Application Information

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IPC IPC(8): A61K31/536A61P31/18A61K9/00A61K9/20
CPCY02A50/30
Inventor 余龙陈帅张明君胡海荣
Owner FUDAN UNIV
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