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Preparation method and novel medical application of myricetin derivatives

A technology of derivatives and drugs, applied in the field of medicine, can solve the problems of undiscovered reports on the application of myricetin derivatives

Pending Publication Date: 2020-06-16
CHANGCHUN UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Before the completion of the present invention, there was no literature report that the derivatives of cyclomyricetin have anti-Alzheimer's disease effects, and no reports on the application of myricetin derivatives in the preparation of anti-Alzheimer's disease drugs have been found.

Method used

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  • Preparation method and novel medical application of myricetin derivatives
  • Preparation method and novel medical application of myricetin derivatives
  • Preparation method and novel medical application of myricetin derivatives

Examples

Experimental program
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Embodiment 2

[0041] Embodiment 2 compound 1-16 preparation method

[0042] Dissolve 1mmol myricetin and 1.2mmol amino-containing compound in 20mL of absolute ethanol, add a small amount of glacial acetic acid dropwise, stir and reflux the mixture for 36-48h, check the reaction progress by thin-layer chromatography, and obtain a brown-yellow solution, remove part of it under reduced pressure Ethanol, a yellow solid precipitated, suction filtered, washed the solid with distilled water, and then washed with a small amount of ethanol, dried at room temperature, and recrystallized from absolute ethanol to obtain the corresponding myricetin derivative 1-16. The yields were all greater than 85%.

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Abstract

Myricetin which is obtained by extraction, separation and purification from Ampelopsis grossedentata (Hand.-Mazz.) W.T. Wang is adopted as a lead compound, and is subjected to a condensation reactionwith amino-containing compounds such as phenylhydrazine, benzoyl hydrazine, phenylaminourea, phenylthiosemicarbazide, phenylacetylhydrazine, phenoxyacethydrazide and phenylaminoacethydrazide to obtainmyricetin derivatives. Enzymology and cell tests prove that the myricetin derivatives have a relatively strong effect of inhibiting acetylcholin esterase, so that the effect of preventing and treating Alzheimer's disease is achieved. Further research shows that the activity of most myricetin derivatives is higher than that of the lead compound.

Description

technical field [0001] The invention relates to a series of derivatives of myricetin obtained from natural Chinese medicine as a lead compound through a synthesis reaction, to be exact, a series of derivatives prepared by taking chemical components extracted from traditional Chinese medicine as lead compounds The invention relates to structural modification for the purpose of anti-Alzheimer's disease activity, and belongs to the field of medicine. Background technique [0002] Alzheimer's disease (AD) is a common degenerative disease of the central nervous system characterized by progressive memory loss, cognitive dysfunction, and personality changes in middle-aged and elderly people. Intensified, the global number of Alzheimer's patients has exceeded 35 million, which will bring many social and economic problems. Therefore, the prevention and treatment of AD has become a very urgent social and medical problem. At present, there are many kinds of drugs for the treatment of...

Claims

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Application Information

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IPC IPC(8): C07D311/68A61P25/28
CPCC07D311/68A61P25/28
Inventor 赫玉芳段明华李海燕于露宁春雪姚佩欣南敏伦
Owner CHANGCHUN UNIV OF CHINESE MEDICINE
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