Application of chrysin derivative in medicine preparation

A technology for preparing medicines and uses, applied to the application field of chrysin derivatives in the preparation of medicines, and can solve the problems of poor solubility, complex pathology, difficult treatment and the like

Pending Publication Date: 2021-12-10
SHENZHEN FENGYU BIOMEDICAL TECH CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A large number of studies have shown that with the development of the economic level, the change of lifestyle, the adjustment of diet structure, and the influence of genetic factors, diseases characterized by abnormal lipid metabolism, such as obesity, dyslipidemia, fatty liver, atherosclerosis, etc. The incidence of cirrhosis is increasing year by year, and

Method used

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  • Application of chrysin derivative in medicine preparation
  • Application of chrysin derivative in medicine preparation
  • Application of chrysin derivative in medicine preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053]

[0054]Suyang Su (1.0 mmol, 254 mg) and anhydrous potassium (3.5 mmol, 483 mg) were dissolved in anhydrous acetonitrile (20 mL), then 1-chloroformyl-4-piperidine piperidine hydrochloride (1.0 mmol) , 267mg), stirring reflux for 8 hours; after the reaction, the carnovic drying solvent was decompressed, and 50 ml of water was added. After three extraction of 120 ml of dichloromethane, the organic layer was combined, dried over anhydrous sodium sulfate, filtered, concentrated, obtained The residue was purified by silica gel column chromatography (dichloromethane: methanol = 20: 1) obtained 400 mg, yield 89%. 1 H NMR (400MHz, CDCL 3 Δ12.67 (S, 1H), 7.88 (DD, J = 8.0, 1.4 Hz, 2H), 7.59-7.47 (M, 3H), 6.90 (D, J = 2.1Hz, 1H), 6.71 (S, 1H ), 6.58 (d, j = 2.0 Hz, 1H), 4.35 (D, J = 12.9 Hz, 2H), 2.95 (DT, J = 24.8, 12.6Hz, 2H), 2.78-1.68 (M, 4H), 1.64 (D, J = 11.9 Hz, 2H), 1.51 (D, J = 4.9 Hz, 2H), 1.39-1.27 (m, 2H). 13 C NMR (101MHz, CDCL 3 ) Δ182.88,164.59,161.73,156.90,156.74,1...

Embodiment 2

[0057]

[0058] Suyang (1.0 mmol, 254 mg) and anhydrous potassium (3.5 mmol, 483 mg) were dissolved in anhydrous acetonitrile (20 mL), then N, N-dimethylal chloride (1.0 mmol, 107.5 mg), warming reflux After stirring for 8 hours; after the reaction, the carnovic solvent was subjected to 50 ml of water, and the mixture was added three times with 120 ml of dichloromethane. After combining the organic layer, dried over anhydrous sodium sulfate, filtered, concentrated, the obtained residue silica gel column Purification (dichloromethane: methanol = 100: 1) obtained product 300 mg, yield 92%. 1 H NMR (400MHz, CDCL 3 Δ12.68 (S, 1H), 7.88 (DD, J = 8.0, 1.4 Hz, 2H), 7.59-7.49 (M, 3H), 6.93 (D, J = 2.0 Hz, 1H), 6.72 (S, 1H ), 6.60 (D, J = 2.0 Hz, 1H), 3.08 (D, J = 29.5 Hz, 6H). 13 C NMR (101MHz, CDCL 3 Δ182.91, 164.57, 161.74, 157.05, 156.77, 153.49, 132.07, 131.11, 129.16, 126.39, 108.46, 106.06, 106.04, 105.30, 100.92, 100.90, 36.84, 36.61.

Embodiment 3

[0060]

[0061] Suyang (1.0 mmol, 254 mg) and anhydrous potassium (8.0 mmol, 1.1 g) were dissolved in anhydrous acetonitrile (30 mL), then N, N-dimethylachaloyl chloride (5.0 mmol, 537.7 mg), warmed After refluxing for 12 hours; after the reaction was completed, the carnovic solvent was decompressed, and 50 ml of water was added. After 120 ml of dichloromethane, the organic layer was combined, dried over anhydrous sodium sulfate, filtered, concentrated, the resulting residue silicone column Chromatography was purified (dichloromethane: methanol = 50: 1) obtained 350 mg, yield 95%. 1 H NMR (400MHz, CDCL 3 Δ7.84 (DD, J = 7.6, 1.8 Hz, 2H), 7.50 (D, J = 7.0 Hz, 3H), 7.36 (D, J = 2.2 Hz, 1H), 6.92 (D, J = 2.2 Hz, 1H), 6.64 (S, 1H), 3.20 (S, 3H), 3.05 (S, 3H), 3.05 (D, J = 7.1 Hz, 6H). 13 C NMR (101MHz, CDCL 3 δ176.91, 162.21, 157.66, 154.86, 154.59, 153.23, 151.08, 131.58, 131.30, 129.04, 126.16, 114.08, 114.03, 108.63, 106.85, 36.81, 36.58, 36.56.

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Abstract

The invention provides application of a chrysin derivative in medicine preparation. The chrysin derivative has a structure as shown in a formula I, and the biological activity and bioavailability of the chrysin derivative are obviously higher than those of chrysin. The chrysin derivative can be used for preparing medicines for preventing and/or treating hyperglycemia, hyperlipidemia, the Alzheimer disease (AD), senile dementia, the Parkinson disease (PD), amyotrophic lateral sclerosis (ALS), cerebral ischemia, brain injury, obesity, diabetes and/or diabetic complications, diabetic eye diseases, diabetic nephropathy, dyslipidemia, atherosclerosis, fatty liver, non-alcoholic fatty liver disease, cirrhosis, hepatitis, obstructive jaundice, myocardial infarction and the like.

Description

Technical field [0001] The present invention relates to the art of the pharmaceutical, and more particularly to the application of a boarin derivative in the preparation of the drug. Background technique [0002] As Yang Su (5,7-dihydroxy flavonoids) is a flavonoid compound existing in nature, antioxidant, anti-inflammatory, anti-anxious, anti-tumor, anti-diabetic, antibacterial, and other pharmacological activity. [0003] A series of compounds were prepared in the prior art, such as: CN101774994A was prepared to obtain a loblast long chain derivative for the treatment of atherosclerosis. The iodine containment containing iodine derivatives for anti-radiation damage is prepared in CN103896896A. The boarnin derivative was prepared in CN105884735A, which was carried out to the amine methylation reaction, and the obtained derivative had a treatment of hyperuricemia. The preparation of Peerkin derivatives for preventing and treating Koxac viruses. [0004] By detailed research and r...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K31/453A61K31/5377A61K31/496A61P25/00A61P25/28A61P25/16A61P21/00A61P9/10A61P3/04A61P3/10A61P3/00A61P3/06A61P1/16A61P13/12A61P27/02A61P29/00
CPCA61K31/352A61K31/453A61K31/5377A61K31/496A61P25/00A61P25/28A61P25/16A61P21/00A61P9/10A61P3/04A61P3/10A61P3/00A61P3/06A61P1/16A61P13/12A61P27/02A61P29/00
Inventor 杨细飞谢永美李书鹏杨超刘恭平张芮铭叶涛
Owner SHENZHEN FENGYU BIOMEDICAL TECH CO LTD
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