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Diarylmiazines derivatives, preparation method and use thereof

A technology of diarylpyrimidine and derivatives, which is applied in the field of medicine and achieves the effects of novel structure, good anti-HIV biological activity and low cytotoxicity

Inactive Publication Date: 2008-02-13
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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  • Diarylmiazines derivatives, preparation method and use thereof
  • Diarylmiazines derivatives, preparation method and use thereof
  • Diarylmiazines derivatives, preparation method and use thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0036] Embodiment 1: the synthesis of diarylpyrimidine derivatives

[0037] 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.

[0038] 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:

[0039] in N 2Under protection, 1-naphthol (4.2mmol) was added to 30ml of anhydrous DMF, stirred to dissolve it, and then 2-(4-cyanoanilino)-4-chloro-5-methylpyrimidine (3.5mmol ), stirred for 10min to dissol...

Embodiment 2

[0049] Embodiment 2 anti-HIV biological activity test

[0050] 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 .

[0051] Materials and Methods:

[0052] The anti-HIV activity of each compound is monitored by the i...

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Abstract

The present invention discloses a series of diarylpyrimidine derivatives (DAPYs) represented by general formula I, its N-oxides, its pharmaceutically acceptable salts, its stereochemical isomers, its hydrates and solvates, and more Crystals and co-crystals, their precursors and derivatives with the same biological function, their preparation methods and the application of compositions containing one or more of these compounds in the treatment of AIDS and other related drugs.

Description

technical field [0001] The present invention belongs to the technical field of medicine, and specifically relates to the pharmaceutically acceptable salts, hydrates and solvates, polycrystals and cocrystals, and precursors and derivatives of diarylpyrimidine derivatives described in general formula I. , its preparation method and the application of the composition containing one or more such compounds in the treatment of AIDS and other related drugs, its preparation method and use. The series of compounds not only have good anti-HIV-1 virus biological activity, but also show good inhibitory effect on HIV-2 ROD virus strain. 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 beco...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/47A61K31/505A61P31/18
Inventor 陈芬儿冯筱晴
Owner FUDAN UNIV
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