Diaryl pyridine derivatives, preparation method thereof and application thereof

A kind of technology of diarylpyrimidine and derivatives, applied in the field of medicine

Inactive Publication Date: 2009-12-16
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Classical NNRTIs are only effective against HIV-1 virus but not against HIV-2 virus

Method used

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  • Diaryl pyridine derivatives, preparation method thereof and application thereof
  • Diaryl pyridine derivatives, preparation method thereof and application thereof
  • Diaryl pyridine derivatives, preparation method thereof and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Embodiment 1: the synthesis of diarylpyrimidine derivatives

[0028] Under the protection of an inert gas, add the substituted naphthol to an anhydrous aprotic solvent, stir to dissolve it; then add 4-chloropyrimidine derivatives, stir to dissolve it; add anhydrous K 2 CO 3 , control the temperature at 90-100°C, and stir for 8-12 hours. After TLC showed that the reaction was finished, the K 2 CO 3 , the filtrate was poured into cold water, the precipitated solid was filtered and dried. The desired compound can be obtained by column separation or recrystallization.

[0029] Using 4-chloropyrimidine derivatives and different substituted naphthols, the target compounds were respectively prepared by the above method, and some results are as follows:

[0030] in N 2 Under protection, β-naphthol derivatives (4.2mmol) were added to 30mL of anhydrous DMF, stirred to dissolve, and then added 2-(4-cyanoanilino)-4-chloro-5-methylpyrimidine ( 3.5mmol), stirred for 10min to d...

Embodiment 2

[0041] Embodiment 2 anti-HIV biological activity test

[0042] The anti-HIV virus activity at the cell level in vitro was determined by the Rega Institute of Pharmacy at Katholleke University in Belgium, mainly including two aspects: inhibitory activity and cytotoxicity to HIV-infected MT-4 cells. The method is described as follows: make the compound in HIV-infected MT-4 cells, at different times of HIV infection, use the MTT method to measure the protective effect of the drug on the cytopathic changes induced by HIV, and calculate that 50% of the cells are free from HIV-induced cell changes. half effective concentration IC 50 , Toxicity determination is carried out in parallel with anti-HIV activity experiment, also in MT-4 cell culture, the concentration that makes 50% uninfected cells take place cytopathic (CC 50 ), and calculate the selectivity index SI=CC 50 / IC 50 .

[0043] Materials and Methods:

[0044] The anti-HIV activity of each compound is monitored by the i...

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Abstract

The invention belongs to the technical field of medicament, and specifically discloses diaryl pyridine derivatives (DAPYs), a preparation method thereof and an application thereof. A structural formula of the compound is expressed as formula I. The invention also relates to medicinal salts thereof such as hydrochloride, sulfate, tartrate, citrate, fumarate and malate, pharmaceutically acceptable prodrug and derivatives, and the application of a composition containing one or more the compounds in related medicaments for treating AIDS.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a diarylpyrimidine derivative and its preparation method and application. The series of compounds not only have good biological activity against HIV-1 virus and HIV-1 reverse transcriptase, but also show high inhibitory activity against drug-resistant virus strain L103N+Y181C. Background technique [0002] AIDS (AIDS) or Acquired Immune Deficiency Syndrome (Acquired Immune Deficiency Syndrome) is an epidemic infectious disease caused by Human Immunodeficiency Virus (HIV). [0003] Reverse transcriptase (Reverse transcriptase, RT) plays a decisive role in the process of HIV reverse transcription from mRNA to DNA, so it has become one of the important targets for the design of anti-AIDS drugs. [0004] In the existing anti-HIV drug research, non-nucleoside reverse transcriptase inhibitors (NNRTIs) have become one of the hotspots of medicinal chemists in various countr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/47A61K31/505A61P31/18
Inventor 陈芬儿梁永宏曾兆森
Owner FUDAN UNIV
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