2-hydroxyl chalcone compound as well as preparation method and purpose thereof

A hydroxychalcone and compound technology, which is applied to a class of 2-hydroxychalcone compounds, the fields of preparation and use thereof, and can solve the problems of unsatisfactory depolymerization activity, poor curative effect, weak inhibitory effect and the like

Active Publication Date: 2016-04-13
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In previous studies, we designed and synthesized scutellarin aglycon carbamate derivatives (CN101337956A, CN102603698A), stilbene or ethane carbamate for the acetylcholinesterase and oxidative stress factors in the pathogenesis of AD Ester compounds (CN102816090A), isoflavone carbamate compounds (CN102827131A), flavonoid alkylamine compounds (CN103087024A), genistein alkylamine compounds (CN103113340A), stilbene oxyalkylamine compounds (CN103073440A), although these compounds have good acetylcholinesterase inhibitory and antioxidant activities, but for Aβ 1-42 Inhibition of self-aggregation was weak (its IC 50 greater than 20.0μM), for Cu 2+ induced Aβ 1-42 Inhibition of aggregation (inhibition rate at 25.0μM concentration is less than 65.0%) and the effect on Cu 2+ induced Aβ 1-42 The aggregation disaggregation activity (the disaggregation rate at 25.0μM concentration is all less than 60.0%) is not ideal, resulting in poor efficacy of these compounds on AD in transgenic animal models

Method used

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  • 2-hydroxyl chalcone compound as well as preparation method and purpose thereof
  • 2-hydroxyl chalcone compound as well as preparation method and purpose thereof
  • 2-hydroxyl chalcone compound as well as preparation method and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 12

[0034] Example 12-hydroxyl ketones (i) preparation method

[0035] Add the corresponding 2-hydroxybenzhenylene compounds (2), 3.0mmol corresponding benzaldehyde compounds (1) and 30ml ethanol in the reaction bottle to the reaction bottle. After mixing well, add 30%KOH aquatic solution 8.0 mmol to the temperature.Return stirring reaction 3.0 to 24.0 hours (tracked with TLC); after the reaction process is completed, it is cooled to room temperature, and the pH is most acidic with 10%hydrochloride solution, and then the pH is used to regulate the pH to the weak alkali with saturated sodium bicarbonate aquatic solution.Sexual, reducing degradation, reducing ethanol, adding 80ml of removal water to the residual liquid, three times with 240ml dichloromethane, washed three times after the organic layer merged with saturated sodium chloride solution, dried after drying sodium sulfateIn addition to the solvent, the residue is purified by the column layer (elute: dichloromethane: acetone = ...

Embodiment 22

[0073] Example 22-hydroxyl ketones (i) and acid-forming preparation method

[0074] Add 2-hydroxyl ketones (i) 2.0 mmol and acetone 50ml in the reaction bottle according to the above-mentioned Example 1, and add 8.0 mmol to the corresponding acid after stirring.By room temperature, decompress the solvents, residual substances with acetone, and the solids filtered out of the solid, that is, the salt of 2-hydroxyl ketones (i). 1 HNMR and ESI-MS are confirmed.

Embodiment 3

[0075] Example 3-biological activity screening results of 2-hydroxyl ketones (i)

[0076]

[0077] a The suppression rate at a concentration of 25.0 μm.

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Abstract

The invention discloses a novel 2-hydroxyl chalcone compound (I), as well as pharmacy acceptable salt, preparation method, medical composition, and purpose thereof in preparing medicines for treating and/or preventing neurodegenerative diseases including but not limited to vascular dementia, Alzheimer's diseases, Parkinson's diseases, Huntington's diseases, dementia relevant to HIV, multiple sclerosis, amyotrophic lateral sclerosis, neuropathic pain, glaucoma and the like (As shown in the description.).

Description

Technical field [0001] The invention is the field of pharmaceutical chemistry, involving a new type of 2-hydroxyl ketone (i) and its acceptable salt, its preparation methods, pharmaceutical compositions, and in preparation therapy and / or prevent neurodegenerationabilityThe use in related diseases, including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Henton, HIV -related dementia, multiple sclerosis, cargo cable sclerosis, neurotic pain, Glaucoma and other neurodegeneration diseases. Background technique [0002] Alzheimer'sDisease (AD, Alzheimer's) is a central nervous system degenerative disease with a central nervous system, which is mainly based on cognitive dysfunction and memory damage.High incidence of cardiovascular disease and cancer, in developed countries such as Europe and the United States, have risen to the fourth place for death.According to the World Health Organization report, 10%of the elderly over the world have 10%intellectu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C225/22C07C221/00C07D295/088C07D211/14C07D295/112A61K31/138A61K31/495A61K31/4453A61K31/445A61K31/40A61K31/5375A61P25/28A61P25/14A61P25/16A61P31/18A61P25/00A61P25/04A61P27/06
Inventor 邓勇谭正怀桑志培李岩刘强肖柑媛强晓明
Owner SICHUAN UNIV
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