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Drug application of N2,N5-bi[2-(3,4-imethoxyphenyl)ethyl]-2,5-pyridine carboxamide

A technology of dimethoxyphenyl and pyridinecarboxamide, 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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  • Drug application of N2,N5-bi[2-(3,4-imethoxyphenyl)ethyl]-2,5-pyridine carboxamide

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Embodiment 1 compound anti-HIV-1 virus increment test

[0041] 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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PUM

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Abstract

The invention discloses application of a micromolecular compound with HIV (Human Immunodeficiency Virus) resisting activity to preparing drugs for resisting AIDS, relating to the field of biomedicine. The world health organization (WHO) and governments around the world highly pay attention to AIDS called as present pestilence and super cancer, however, so far, effective drugs capable of curing the AIDS do not exist. The invention provides application of N2,N5-bi[2-(3,4-imethoxyphenyl)ethyl]-2,5-pyridine carboxamide to preparing the drugs for resisting the AIDS. The N2,N5-DI[2-(3,4-imethoxyphenyl)ethyl]-2,5-pyridine carboxamide has the capability of inhibiting the replication of HIV-1 virus and is designed by aiming at cell target points without easily generating drug resistance as well as is suitable for the medication demands of the AIDS patients for life.

Description

technical field [0001] The invention relates to the field of biomedicine, and relates to the application of a small molecular compound 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 core of viruses, and other...

Claims

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Application Information

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IPC IPC(8): A61K31/44A61P31/18
Inventor 余龙陈帅张明君胡海荣
Owner FUDAN UNIV
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