Application of phenylpropylthiophene derivative in preparation of anti-HIV medicament

A technology of phenylpropylthiophene and HIV, which can be used in antiviral agents, resistance to vector-borne diseases, and pharmaceutical formulations, and can solve problems such as poor curative effect

Inactive Publication Date: 2010-11-24
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 phenylpropylthiophene derivative in preparation of anti-HIV medicament

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 relates to the bio-medicinal field, and relates to application of a phenylpropylthiophene derivative in preparation of an anti-HIV medicament, in particular to application of a small molecular compound with anti-HIV activity in preparation an anti-HIV medicament. The world health organization and each government pay high attention to HIV named as 'contemporary plague' and 'super cancer', but an effective medicament for healing the HIV is not discovered so far. The invention provides application of 2-({6-[(3-carbonyl-4,5,6,7-tetrahydro-1-phenylpropylthiophene-2-group) amino]-6-oxoacetyl} amine)-4,5,6,7-tetrahydro-1-phenylpropylthiophene-3-formic acid in preparation the anti-HIV medicament. The compound has the capability of inhibiting HIV-1 virus replication, is a medicament designed aiming at a cell target, is not easy to form medicament resistance, and meets the requirement of an AIDS patient for lifelong medication.

Description

technical field [0001] The invention relates to the field of biomedicine, and relates to the application of a phenylpropylthiophene derivative in the preparation of anti-AIDS drugs. The phenylpropylthiophene derivative is a small molecular compound with anti-HIV activity. 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 polyprote...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/381A61P31/18
CPCY02A50/30
Inventor 余龙张明君陈帅胡海荣
Owner FUDAN UNIV
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