Nitrogen-containing polyhydroxy fragrant compounds, preparation and uses thereof

A compound and polyhydroxyl technology, which is applied in the field of nitrogen-containing polyhydroxyaromatic compounds and their preparation, can solve the problems of incomplete eradication of viruses in the body, high price, and limited efficacy, and achieve the effect of improving integrase inhibitory activity and selectivity
CN101429142AInactive Publication Date: 2009-05-13SHANDONG UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANDONG UNIV
Publication Date
2009-05-13
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a nitrogen-containing polyhydroxy arometic compound having a structure as shown in a general formula 1, wherein R1 is hydrogen, methyl or fluorine; R2 is hydrogen, methyl, acetyl, fluorine, chlorine or bromine; R3 is hydrogen, methyl, butyl, methoxyl, ethoxyl, fluorine, chlorine, bromine or nitro; R4 is hydrogen, methyl, acetyl, fluorine, chlorine or bromine; and n is 0 or 1. The invention also relates to a method for preparing the nitrogen-containing polyhydroxy arometic compound in the general formula 1. The compound has obvious inhibitory activity to HIV integrase, and is used for preparing anti-AIDS medicine. The n is equal to 0 or 1.
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Description

Technical field

[0001] The invention relates to the field of organic compound synthesis and medical applications, in particular to nitrogen-containing polyhydroxy aromatic compounds and their preparation methods and pharmaceutical applications. Background technique

[0002] Human immunodeficiency virus (HIV) is the pathogen of AIDS (acquired immune deficiency syndrome, AIDS), divided into HIV1 and HIV-2 types. HIV-1 is prevalent all over the world, and HIV-2 is mainly confined to western Africa. HIV-1 replication requires three key enzymes: reverse transcriptase, protease and integrase. The current drugs for the treatment of AIDS mainly target reverse transcriptase and protease to prevent reverse transcription of single-stranded RNA viruses or inhibit viral protein cleavage and mature virus release. Since reverse transcriptase and protease are highly susceptible to mutations, the effectiveness of these drugs is limited by the rapid emergence of drug resistance. Antiviral combinat...

Claims

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