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A kind of α-glucosidase inhibitor and its application

A technology of glucosidase and inhibitor, which is applied in the field of medicine to achieve the effects of significantly inhibiting activity, improving selectivity, and enhancing drug efficacy

Active Publication Date: 2021-06-08
WUYI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no relevant report on its application in inhibiting glucosidase

Method used

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  • A kind of α-glucosidase inhibitor and its application
  • A kind of α-glucosidase inhibitor and its application
  • A kind of α-glucosidase inhibitor and its application

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Experimental program
Comparison scheme
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Embodiment 1

[0042] Embodiment 1 of the present invention is: an α-glucosidase inhibitor, the active ingredient of which is 3-cinnamoyl-coumarin (3-cinnamoyl-2H-chromen-2-one), whose structural formula as follows: (labeled 3a).

[0043] Prepared with reference to the above steps, in the formula, R is The yield was 51.7%, and the obtained product was in the form of a yellow solid, and its structure was characterized by nuclear magnetic resonance (Nuclear Magnetic Resonance, NMR), and the results were as follows: 1 H NMR (500MHz, CDCl 3 )δ8.60(s,1H),7.92(dd,J=40,20Hz,2H),7.71-7.65(m,4H),7.44-7.39(m,4H),7.35(t,J=8,7.5 Hz,1H).

[0044] Embodiment 2 of the present invention is: an α-glucosidase inhibitor whose active ingredient is (E)-3-((p-tolyl)acryloyl)-coumarin ((E)-3-(3 -(p-tolyl)acryloyl)-2H-chromen-2-one), labeled 3b.

[0045] Prepared with reference to the above steps, in the formula, R is Its productive rate is 45.9%; The product obtained is a yellow solid, and its structure ...

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Abstract

The present invention discloses an α-glucosidase inhibitor and its application. The α-glucosidase inhibitor includes compounds of the following structural formula: wherein, R is selected from thienyl, indolyl, substituted or unsubstituted phenyl . The scheme of the present invention cleverly utilizes the principle of skeleton splicing to splice the active units of coumarin and chalcone with different targets, so that it can not only enhance the efficacy of the drug, but also improve the selectivity of the interaction between the drug and the target; the inhibitor The active ingredients of the invention not only have low toxicity, but also can effectively inhibit the activity of α-glucosidase, and have good potential medical care value.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an alpha-glucosidase inhibitor and application thereof. Background technique [0002] Drastic changes in work patterns, improvements in transportation, lack of physical activity, dramatic changes in lifestyle, and junk food accompanying globalization have led to a dramatic increase in the incidence of diabetes worldwide in the last century. According to the latest data of diabetes epidemiology in China released by JAMA magazine, the results show that the prevalence rate of adult diabetes is 10.9% (95% CI, 10.4%-11.5%) and the proportion of pre-diabetes is as high as 35.7% (95% CI, 34.1%-37.4%). %). In addition, according to related reports (http: / / www.bjd.com.cn / a / 201911 / 09 / WS5dc627d7e4b0621d5c14d277.html), only 36.5% of all diabetic patients knew that they had diabetes, and 32.2% of people are receiving treatment. Among the treated patients, only less than half (49.2%) had e...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/366A61K31/381A61K31/404A61P3/10A23L33/10
CPCA23V2002/00A61K31/366A61K31/381A61K31/404A23L33/10A61P3/10A23V2200/328
Inventor 徐学涛陈洁林芷晴李冬利张焜
Owner WUYI UNIV