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Application of 4-acetyldiazenequinoline derivative in preparing anti-AIDS drugs

An acetyldiazene quinoline, anti-AIDS technology, applied in antiviral agents, pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve the problems of anti-HIV drugs that have not been reported, and the long time

Inactive Publication Date: 2010-09-22
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] The third category is used for cell infection. Different antibiotics are selected according to bacteria and drug sensitivity tests. The treatment of atypical mycobacterium avium infection is the same as that of anti-tuberculosis, but the time is slightly longer
[0016] The fourth category is antiviral infection drugs, there is no specific drug yet, mainly rely on symptomatic treatment, commonly used are acyclovir, famciclovir, etc.
[0017] Yet, so far, no one has reported that the compounds of the present invention are used for the preparation of anti-HIV virus medicaments

Method used

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  • Application of 4-acetyldiazenequinoline derivative in preparing anti-AIDS drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1 compound anti-HIV-1 virus increment test

[0035] 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 cells with 100 50% tissue infection equivalents, and at the same time, different concentration gradients of compounds (FD8, Interchim Company, AK-968 / 15603640) were added and cultured overnight (wells without compounds were used as blank controls). 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, then measure the p24 protein content by ELISA (p24 is the coat protein of HIV-1, which can be used as a measure of the number of virions index of). Coat the plate with anti-HIV immunoglobulin overnight (pH 9.6 carbonic acid buffer, 4°C), then add PBS containing 4% skimmed milk powder to block; add 100uL virus lysa...

Embodiment 2

[0037] Example 2 Toxicity test of small molecule compounds on MT-2 cells:

[0038] 2.1 Plant 5×10 in a 24-well plate 5 / well of MT-2 cells.

[0039] 2.2 Infect the cells with HIV-1IIIB virus particles at a multi-infection index (MOI) of 0.01, and culture them in a cell culture incubator at 37° C. for 1 hour.

[0040] 2.3 Wash the cells twice with PBS.

[0041] 2.4 The small molecular compound (Interchim, AK-968 / 15603640) was diluted with RPMI 1640 medium containing 10% fetal bovine serum to a final concentration of 10 μM, and added to the infected cells. Incubate for 48 hours at 37°C in a cell culture incubator.

[0042] 2.5 Fix the cells with PBS solution containing 1% formaldehyde, and detect the expression of HIV-1p24 protein in the cells with FITC-coupled anti-p24 antibody. The number of p24+ cells was measured by flow cytometry. Inhibition rate%=[1-(E-N) / (P-N)]×100%. E represents the number of p24+ cells in the presence of the compound, P and N represent the positiv...

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Abstract

The invention belongs to the genetic engineering and chemical fields and relates to the application of 4-acetyldiazenequinoline derivative in preparing anti-AIDS drugs. Since AIDS is discovered firstly in 1981, methods and drugs are not developed successfully until now in medical field. The invention provides the application of a small molecular compound of 1-(2-(3-ethoxyphenyl)quinoline-4-yl)-2-((4-methoxyl-3-(morpholinylmethy)phenyl)diazenyl)ethyl ketone in preparing anti-AIDS drugs. A small molecular ligand FD8 screened by the invention has stronger antiviral ability and less toxicity to host cells, thereby being an ideal anti-HIV-1 lead compound.

Description

technical field [0001] The present invention relates to the fields of chemical industry and medicine, and relates to the application of 4-acetyldiazene quinoline derivatives in the preparation of anti-AIDS drugs, in particular to the 1-[2-(3-ethyl 4-acetyldiazene quinoline derivatives Application of oxyphenyl) quinoline-4-yl]-2-{[4-methoxy-3-(morpholinemethyl)phenyl]diazene}ethanone in the preparation of anti-AIDS drugs. Background technique [0002] Since AIDS (AIDS) was first discovered in 1981, the medical community has not yet successfully developed a method for completely treating AIDS, nor has it successfully produced a vaccine to prevent human immunodeficiency virus (HIV, also known as HIV) infection. Many medicines and methods for inhibiting reverse transcriptase (RT), blocking the replication of HIV, and slowing down the growth rate of the virus have been developed. Anti-AIDS drugs mainly fall into the following categories: [0003] 1 Antiretroviral drugs [0004...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61P31/18
Inventor 余龙陈帅张明君
Owner FUDAN UNIV
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