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2-arylmethylthio-6-(tetrahydroquinoline-1-methyl)-4-pyrimidinone derivatives and their preparation methods and applications

A technology of arylmethylthio and tetrahydroquinoline, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, organic chemistry, etc., and can solve problems such as loss of clinical potency

Inactive Publication Date: 2011-12-21
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the spread of drug-resistant strains, this type of drug rapidly loses its clinical efficacy

Method used

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Embodiment 22

Embodiment 32

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Abstract

The present invention provides a 2-[(substituted phenylamino)carbonylmethylthio]-6-(2,6-dichlorobenzyl)-3H-pyrimidin-4-one derivative, the general structural formula I is as follows: Where R1 is: H, methyl or ethyl; R2 is: 2-bromoacetophenone, p-methyl-2-chloroacetophenone, p-chloro-2-chloroacetophenone, p-nitro- 2-chloroacetophenone, p-cyano-2-chloroacetophenone, p-methoxy-2-chloroacetophenone, p-fluoro-2-chloroacetophenone, benzyl bromide, p-methyl Benzyl chloride, p-chlorobenzyl chloride, p-nitrobenzyl chloride, p-cyanobenzyl chloride, p-methoxybenzyl chloride or p-fluorobenzyl chloride. The invention also relates to a preparation method of the compound and its application as an HIV inhibitor.

Description

technical field The invention relates to a derivative and a preparation method thereof, in particular to 5-alkyl-2-arylmethylthio-6-[(1,2,3,4-tetrahydroquinoline)-1-methyl] The invention relates to 3H-pyrimidin-4-one derivatives and their preparation method and application, which belong to the technical field of organic compound synthesis and medical application. Background technique AIDS (AIDS) is an infectious disease caused by human immunodeficiency virus (HIV), which seriously affects human life and health. HIV is a retrovirus, and the important role of reverse transcriptase in the viral life cycle makes it an important target for antiviral therapy. There are two classes of reverse transcriptase inhibitors: nucleoside reverse transcriptase inhibitors and non-nucleoside reverse transcriptase inhibitors. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have attracted much attention due to their high efficiency, low toxicity, and high selectivity. However, due to...

Claims

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Application Information

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IPC IPC(8): C07D401/06A61K31/506A61P31/18
Inventor 刘新泳张静展鹏
Owner SHANDONG UNIV
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