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Compound, and preparation method and application thereof

A compound, drug technology, applied in the field of biochemistry

Inactive Publication Date: 2014-12-17
UNIV OF SCI & TECH OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there are no drugs and therapies that can effectively treat AIDS in the world, and only drugs can be used to properly control the proliferation of HIV in the human body

Method used

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  • Compound, and preparation method and application thereof
  • Compound, and preparation method and application thereof
  • Compound, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] 1, prepare compound shown in formula I of the present invention (R 1 for -H,R 2 for -CH 3 , R 3 for -H,R 4 for -H,R 5 for -H,R 6 for -(CH 2 ) 3 -NH 2 , X is Cl)

[0041] 3mmol of the compound shown in formula II was dissolved in 20mL CH 2 Cl 2 , add 6mmol m-chloroperoxybenzoic acid (m-CPBA), stir and react at room temperature for 17 hours column chromatography to separate the compound shown in formula III; 3 Refluxed in isopropanol for 8 hours, and then separated by column chromatography to obtain the compound shown in formula I.

[0042] The reaction formula is as follows:

[0043]

[0044] The compound prepared 1 H nuclear magnetic resonance (300MHz) detection, the solvent is D 2 O, test results see figure 1 , the results show that the prepared compound is consistent with the structure shown in formula I.

[0045] 2. Cytotoxicity test and HIV inhibition test materials

[0046] The human T lymphocyte line C8166 and the HIV-1 experimental strain HIV...

Embodiment 2

[0055] 1, prepare compound shown in formula I of the present invention (R 1 for -H,R 2 for-Br, R 3 for -H,R 4 for -H,R 5 for -H,R 6 for -(CH 2 ) 3 -NH 2 , X is Cl)

[0056] 3mmol of the compound shown in formula II was dissolved in 20mL CH 2 Cl 2 In, add 6mmol m-chloroperoxybenzoic acid (m-CPBA), stir and react at room temperature for 12 hours column chromatographic separation to obtain the compound shown in formula III; the compound shown in 1mmol formula III, the compound shown in 5mmol formula IV and the NaHCO of 2mmol 3 Refluxed in isopropanol for 6 hours, and then separated by column chromatography to obtain the compound shown in formula I.

[0057] The reaction formula is as follows:

[0058]

[0059] The compound prepared 1 H nuclear magnetic resonance (300MHz) detection, the solvent is D 2 O, test results see figure 2 , the results show that the prepared compound is consistent with the structure shown in formula I.

[0060] 2. Cytotoxicity test and H...

Embodiment 3

[0064] 1, prepare compound shown in formula I of the present invention (R 1 for -H,R 2 for -CH 3, R 3 for -H,R 4 for -H,R 5 for -H,R 6 for -(CH 2 ) 4 -NH 2 , X is Cl)

[0065] 3mmol of the compound shown in formula II was dissolved in 20mL CH 2 Cl 2 , add 6mmol m-chloroperoxybenzoic acid (m-CPBA), stir and react at room temperature for 20 hours column chromatography to separate the compound shown in formula III; the compound shown in 1mmol formula III, the compound shown in 5mmol formula IV and the NaHCO of 2mmol 3 Refluxed in isopropanol for 10 hours, and then separated by column chromatography to obtain the compound shown in formula I.

[0066] The reaction formula is as follows:

[0067]

[0068] The compound prepared 1 H nuclear magnetic resonance (300MHz) detection, the solvent is D 2 O, test results see image 3 , the results show that the prepared compound is consistent with the structure shown in formula I.

[0069] 2. Cytotoxicity test and HIV inhib...

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Abstract

The invention relates to the biochemical field, and discloses a compound. The structure of the compound is represented by formula I. The compound of the formula I treats host conservation cell proteins PCAFBRD as an action target, can latently solve a drug resistance problem caused by the high HIV variation, has a good HIV propagation inhibition activity, has a low toxicity to human normal lymphocytes, and can be applied to the preparation of drugs for inhibiting the HIV propagation.

Description

technical field [0001] The present invention relates to the field of biochemistry, and more specifically relates to a compound and its preparation method and application. Background technique [0002] AIDS, Acquired Immunodeficiency Syndrome, is an infectious disease caused by human immunodeficiency virus (HIV) infection. HIV is a virus that attacks the body's immune system. It takes the most important T4 lymphoid tissue in the human immune system as an attack target, destroys T4 lymphoid tissue in large quantities, and produces highly fatal internal failure. This virus spreads throughout the region for life, destroys the immune balance of people, and makes the human body a carrier of various diseases. [0003] HIV itself does not cause any disease, but when the immune system is destroyed by HIV, the human body loses the opportunity to replicate immune cells due to low resistance, and is infected with other diseases, resulting in various co-infections and death. [0004] ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/90A61K31/4412A61K31/5377A61P31/18
Inventor 汪志勇王强姚雪彪郑永唐郑媛
Owner UNIV OF SCI & TECH OF CHINA