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Icariin derivatives and their preparation methods and uses

A technology of icariin and derivatives is applied in the preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., to achieve the effect of excellent medicinal effect

Inactive Publication Date: 2016-04-20
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] If new cholinesterase inhibitors can be found by improving the structure of icariin, it will bring good news to the treatment of Alzheimer's disease

Method used

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  • Icariin derivatives and their preparation methods and uses
  • Icariin derivatives and their preparation methods and uses
  • Icariin derivatives and their preparation methods and uses

Examples

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Embodiment 1

[0025] Embodiment 1 Preparation of icariin derivatives of the present invention

[0026] Take 0.5g (0.74mmol, 1equiv) ICA in a 50mL flask, add 10mL of methanol and stir to form a suspension for later use, add 37% formaldehyde solution (10equiv) to another 50mL flask, dilute with 2mL of methanol, add dropwise under stirring ( 0.74mmol, 1equiv) secondary ammonia (structural formula is as follows), stirred at room temperature for 10min, then slowly added dropwise the methanol suspension of ICA to the flask, heated to reflux for 12h, TLC monitoring, after the reaction was completed, concentrated in vacuo, the crude product was dissolved In ethyl acetate, washed with saturated brine, then washed with water, dried over anhydrous MgSO4, concentrated in vacuo, and column chromatographed to obtain the nitrogen-containing derivatives of icariin corresponding to secondary ammonia.

[0027] The structural formula of the above-mentioned secondary ammonia is Among them, R 1 , R 2 is eth...

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Abstract

The invention provides icariin derivatives disclosed in the specification, wherein R1 and R2 are respectively and independently selected from H and C1-C5 alkyl groups, or R1 and R2 with N connected with R1 and R2 jointly form a substituted or non-substituted 3-6-element ring or a 3-6-element ring containing more than two heteroatoms; and the substituent group is selected from C1-C5 alkyl groups. The icariin derivatives provided by the invention have in-vitro acetylcholine ester inhibiting activity, and have better drug effects than icariin, thereby providing a new option for clinical medicines for treating senile dementia.

Description

technical field [0001] The present invention relates to icariin derivatives and their preparation method and use. Background technique [0002] The most common form of dementia is Alzheimer's disease (AD), a progressive neurodegenerative disorder that is one of the most common causes of mental deterioration in middle-aged and older adults, with more than 250,000 people living with Alzheimer's disease. In the past few decades, a large amount of research work has been dedicated to exploring the pathogenesis of Alzheimer's disease and seeking drugs for the treatment of Alzheimer's disease, and various hypotheses have been put forward one after another, among which the latest and most mainstream hypothesis is the theory of beta-amyloid deposition (Aβ). However, there is no new drug based on this theory on the market. At present, three new phase III clinical drugs targeting Aβ have been declared a failure, which is a blow to the Aβ theory. At present, there are still many drug...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H17/07C07H1/00A61K31/706A61K31/7056A61K31/7048A61P25/28
Inventor 尹述凡李霞陈超董林李颖
Owner SICHUAN UNIV
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