Diaryl pyrimidine derivative, preparation method and use thereof

A technology of diarylpyrimidine and derivatives is applied in the field of medicine and achieves the effects of low cytotoxicity, novel structure and simple preparation method

Inactive Publication Date: 2010-06-30
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Classical NNRTIs only work on HIV-1, but not HIV-2, study shows

Method used

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  • Diaryl pyrimidine derivative, preparation method and use thereof
  • Diaryl pyrimidine derivative, preparation method and use thereof
  • Diaryl pyrimidine derivative, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1 synthesis of diaryl pyrimidine derivatives

[0038]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. Decolorized by activated carbon and recrystallized from toluene to obtain the desired compound.

[0039] Different 4-chloropyrimidine derivatives and different substituted naphthols were used to obtain the target compounds by the above method, and some results are as follows:

[0040] in N 2 Under protection, 8-hydroxyquinoline (4.2mmol) was added to 30mL of anhydrous DMF, stirred to dissolve it, and then 2-(4-cyanoanilino)-4-chloro-5-methylpyrimidine (3.5 mmol), stirred for 10min to di...

Embodiment 2

[0058] Embodiment 2 anti-HIV biological activity test

[0059] 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 EC 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 / EC 50 .

[0060] The anti-HIV activity of each compound is monitored by the inhibitory effect of the drug on t...

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PUM

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Abstract

The invention belongs to the technical field of medicines and relates to a diaryl pyrimidine derivative of the general formula I, medicinal salts thereof, hydrates and solvolytes thereof, polycrystal and eutectic thereof, and precursors and derivatives thereof with the same biological functions, a preparation method thereof, application of combination containing one or more compounds in relative medicines for treating acquired immune deficiency syndrome and the like, a preparation method and use of the combination. Experimental results show that the compound of the invention not only has excellent biological activity of resisting HIV-1 virus and relatively small cytotoxicity, but also shows relatively good inhibitory action to a drug-resistant virus strain L103N+Y181C, can be used as medical candidate resisting the HIV and can be further developed as a medicine resisting AIDS.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to diarylpyrimidine derivatives. It specifically relates to the pharmaceutically acceptable salts of diarylpyrimidine derivatives described in general formula I, their hydrates and solvates, their polycrystals and co-crystals, their precursors and derivatives with the same biological function, their preparation methods and containing a The application of or the composition of a plurality of such compounds in the treatment of related drugs such as AIDS and its preparation method and application. Background technique [0002] AIDS (AIDS) or Acquired Immune Deficiency Syndrome (Acquired Immune Deficiency Syndrome) is an epidemic infectious disease caused by Human Immunodeficiency Virus (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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12C07D239/47A61K31/506A61K31/505A61P31/18
Inventor 陈芬儿梁永宏曾兆森
Owner FUDAN UNIV
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