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Application of 2-cycloxyl substituted or cyclothio substituted hydroxyacetophenone in treatment of metabolic disease

A technology of metabolism and hydroxyl, which is applied in the field of medicine and can solve problems such as low activity

Active Publication Date: 2012-09-05
NAT INST OF BIOLOGICAL SCI BEIJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among the three hydrogen bonds formed between FTO and 3-methylated thymidine, two play an important role in distinguishing different base specificities: one is between R96 and the O of 3-meT 2 The hydrogen bond formed, the other is the amino N atom of the Glu234 backbone and the O of 3-meT 4 The hydrogen bond formed, due to the chemical composition and steric hindrance of other bases, has only partial activity on C, but only very low activity on A and G

Method used

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  • Application of 2-cycloxyl substituted or cyclothio substituted hydroxyacetophenone in treatment of metabolic disease
  • Application of 2-cycloxyl substituted or cyclothio substituted hydroxyacetophenone in treatment of metabolic disease
  • Application of 2-cycloxyl substituted or cyclothio substituted hydroxyacetophenone in treatment of metabolic disease

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0154] FTO enzyme activity reaction system:

[0155]

[0156] Add 2 μl substrate 3-meT (1.0 mg ml-1), 2 μl wild-type hFTO (5.0 mg ml-1), 2 μl inhibitor (1.0 mg ml-1) to 100 μl reaction system, and incubate at 16°C for 12 hours. The reaction solution was 50 mM 2-N-morpholinoethanesulfonic acid hydrate (MES solution) pH 6.0, 0.2 mM (NH 4 ) 2 FeSO 4 , 1.0 mM 2-ketoglutarate, 2.0 mM ascorbic acid vitamin C.

[0157] The reaction result detector is a Waters automatic purification LC / MS system detector. The results of the reaction are shown in the accompanying drawings and the table below.

[0158]

[0159]

[0160]

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Abstract

The invention discloses an application of 2-cycloxyl substituted or cyclothio substituted hydroxyacetophenone in treatment of metabolic diseases. In particular, the invention relates to an application of a compound as shown in general formula (I) in preparation of medicaments for preventing or treating metabolic diseases. Wherein X is selected from H, NO2, or OH; Y is selected from H or OH; Z is selected from O or S; A ring is selected from an alicyclic group, a heteroalicyclic group, an aryl, and a heteroaryl; Z and R can be connected with any appropriate connection site on the A ring; R represents one or more than one substituent. The metabolic diseases comprise metabolic syndrome, obesity, diabetes mellitus, hyperglycemia, diabetic nephropathy, hyperlipidemia, hypertension, coronary heart diseases, atherosclerotic cardiovascular diseases, cardio-cerebrovascular diseases, and diseases of the liver, the kidney, and the thyroid as a result of the above.

Description

technical field [0001] The invention relates to the application of a class of 2-cyclyl oxygen or sulfur substituted hydroxyacetophenone in the preparation of medicines for preventing or treating metabolic diseases, belonging to the technical field of medicine. Background technique [0002] With the rapid development of the global economy, the improvement of living standards, the continuous change of diet structure, and the reduction of physical labor, the incidence of obesity is increasing day by day, becoming the world's most important health problem. According to incomplete statistics, obesity in the world is doubling every five years at an astonishing rate, and the number of cases is roughly 500 million. The number of direct or indirect deaths caused by obesity has reached 300,000 each year, and it may become the number one killer in the 21st century. Obesity, AIDS, drug abuse, and alcoholism are listed as four major social medical problems in the world. [0003] Obesit...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61K31/517A61K31/513A61K31/505A61K31/443A61K31/4412A61K31/4196A61K31/41A61P3/10A61P3/04A61P13/12A61P3/06A61P9/12A61P9/10A61P1/16A61P5/14
Inventor 柴继杰黄牛韩志富彭士明牛天慧
Owner NAT INST OF BIOLOGICAL SCI BEIJING
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