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Use of miconazole and its derivatives as Tgr5 agonists

A technology of TGR5 and derivatives, applied in the field of biopathological diseases and diseases, miconazole, can solve the problems of strong toxic side effects and poor selectivity

Active Publication Date: 2022-06-21
HENAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, steroid agonists still have disadvantages such as poor selectivity and strong toxic side effects.

Method used

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  • Use of miconazole and its derivatives as Tgr5 agonists
  • Use of miconazole and its derivatives as Tgr5 agonists
  • Use of miconazole and its derivatives as Tgr5 agonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: 1-(2-(2,4-Dichlorophenyl)-2-((2,4-dichlorophenyl)methoxy)ethyl)-1H-1,2,4-tris azoles.

[0032]

[0033] The compound preparation method is as follows:

[0034] Step 1: Dissolve 2,2',3'-dichloroacetophenone (1 g, 4.47 mmol) in methanol, cool down to 0 °C in an ice bath, then add sodium borohydride (0.20 g, 5.37 mmol), gradually The reaction was raised to room temperature for 6 h, and the reaction was completed by TLC. 5 mL of saturated ammonium chloride solution was added to quench the reaction, concentrated under reduced pressure to remove methanol, the concentrated solution was extracted with ethyl acetate, dried over anhydrous sodium sulfate, and the concentrated reduction product was 0.91 g. Yield 90.1%.

[0035] The second step: The first step reduction product (1.0g, 4.43mmol) was dissolved in 20mL DMF, then 1,2,4-triazole (0.37g, 5.32mmol) and potassium hydroxide (0.50g, 8.87mmol) were added ), the temperature was raised to 60 °C for 6 h, and the ...

Embodiment 2

[0038] Example 2: 1-(2-(2,4-Dichlorophenyl)-2-((2,4-dichlorophenyl)methoxy)ethyl)-1H-imidazole.

[0039]

[0040] 1 H NMR (400MHz, DMSO-d 6 )δ7.68(d,J=2.1Hz,1H),7.59(d,J=2.0Hz,1H),7.52-7.44(m,2H),7.43-7.32(m,3H),7.05(s,1H) ), 6.85(s, 1H), 5.08(dd, J=6.6, 4.2Hz, 1H), 4.50–4.37(m, 2H), 4.35–4.21(m, 2H).

Embodiment 3

[0041] Example 3: 1-(2-(2,4-Dichlorophenyl)-2-((2,4-dichlorophenyl)methoxy)ethyl)-1H-pyrazole.

[0042]

[0043] 1 H NMR (400MHz, DMSO-d 6 )δ7.66(d,J=10.1Hz,2H),7.53(d,J=6.4Hz,3H),7.44(s,1H),7.35(d,J=7.0Hz,1H),7.21(d, J=7.0Hz, 1H), 6.23(s, 1H), 5.21(m, 1H), 4.34(m, 4H).

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Abstract

The invention belongs to the technical field of medicine, and relates to the new application of miconazole and derivatives thereof in treating diseases and diseases of biopathological processes in which TGR5 participates. The structural formulas of the miconazole and its derivatives are as follows. The miconazole and its analogues can activate TGR5 activity, and can be used for treating or preventing diseases related to the regulation of TGR5 activity.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to new uses of miconazole and derivatives thereof in the treatment of diseases and disorders in biopathological processes involving TGR5. Background technique [0002] TGR5 receptor is a bile acid membrane receptor, which was first discovered by Maruyama and Kawamata in 2002. It consists of 330 amino acids and contains 7 transmembrane domains. It belongs to the GPCR family. TGR5 is mainly distributed in the gallbladder, intestine, adipose tissue, muscle tissue and gallbladder. TGR5 plays an important regulatory role in a variety of physiological processes, such as energy metabolism, immune inflammatory response, hepatobiliary system function, and gastrointestinal system function. [0003] TGR5 receptor is currently the most well-studied in the regulation of energy metabolism. The stimulation of intestinal TGR5 receptor can promote intestinal L cells to secrete GLP-1...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D249/08C07D233/60C07D231/12A61K31/4196A61K31/415A61K31/4174A61P3/00A61P29/00A61P37/00A61P1/16A61P1/00
CPCC07D249/08C07D233/60C07D231/12A61P3/00A61P29/00A61P37/00A61P1/16A61P1/00
Inventor 陈卫东赵世振王艳东叶文凌聂小博彭雯婧李新萍
Owner HENAN UNIVERSITY
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