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A kind of n-(4-benzylpiperidinyl)-ferulamide compound, preparation method and use thereof

A technology of benzyl piperidine and ferulamide, applied in the field of medicine, can solve the problems of worsening AD process, dementia, neuron loss, etc., and achieve the effect of significant inhibitory activity, good Alzheimer's disease, and low toxicity

Inactive Publication Date: 2019-06-18
NANYANG NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, according to the β-amyloid cascade hypothesis, the production and aggregation of oligomeric Aβ in the brain triggers pathogenesis, eventually leading to neuronal loss and dementia, and Aβ can enter mitochondria to induce oxidative stress, while oxidative stress Excited in the brain of AD patients, and promotes Aβ toxicity through the generation of free radicals, further aggravating the AD process

Method used

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  • A kind of n-(4-benzylpiperidinyl)-ferulamide compound, preparation method and use thereof
  • A kind of n-(4-benzylpiperidinyl)-ferulamide compound, preparation method and use thereof
  • A kind of n-(4-benzylpiperidinyl)-ferulamide compound, preparation method and use thereof

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Embodiment 1

[0029] A kind of N-(4-benzylpiperidinyl)-ferulamide compound, its structure is as shown in formula I:

[0030]

[0031] The chemical reaction equation of the preparation of this compound is:

[0032]

[0033] Add ferulic acid 1 (150mg, 0.772mmol), EDCI (3.54g, 0.926mmol), HOBT (178mg, 0.926mmol) and dichloromethane into the reaction flask, stir well and add 4-benzylpiperidine 2 (0.926 mmol), after addition, stirred overnight at room temperature, monitored by TLC; after the reaction was completed, the solvent was evaporated under reduced pressure, water (40mL) was added to the residue, and extracted with dichloromethane (40mL×2). Wash with sodium chloride aqueous solution (40 mL), dry over anhydrous sodium sulfate, filter, evaporate the filtrate to remove the solvent under reduced pressure, and purify the residue by silica gel column chromatography (eluent: petroleum ether / acetone=20 / 1) to obtain the target product N -(4-Benzylpiperidinyl)-ferulamide compound (I).

[00...

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Abstract

The invention discloses an N-(4-benzylpiperidyl)-feruloylagmatine compound, a preparation method and application thereof. The compound has remarkable inhibition activity on self aggregation of butyryl cholinesterase and Abeta1-42, also has very strong antioxidant activity and has an obvious nerve protection function for hydrogen peroxide induced PC12 cell injury, thereby showing that the compound (I) is a multi-target inhibitor. Further in vivo experiments reflect that the compound has a favorable effect for treating the Alzheimer's disease, is low in toxicity and has good clinical application prospects.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an N-(4-benzylpiperidinyl)-ferulamide compound, a preparation method and its use, especially the use in the preparation of drugs for treating Alzheimer's disease. Background technique [0002] Alzheimer's disease (Alzheimer's disease, AD, senile dementia) is a central nervous system degenerative disease mainly characterized by progressive cognitive impairment and memory impairment. With the rapid aging of the global population, the elderly population Health problems have become a major social problem that needs to be solved urgently. Alzheimer's disease (AD) is one of the diseases with the highest morbidity and mortality among the elderly. According to the "2015 Global Alzheimer's Report" released by Alzheimer's Disease International (ADI), more than 46 million people worldwide suffered from dementia in 2015, and it is predicted that by 2050, the global There will be 131.5 million peopl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/16A61K31/445A61P25/28A61P39/06A61P25/00
CPCC07D211/16
Inventor 桑志培柳文敏王柯人潘万里张胜程新峰
Owner NANYANG NORMAL UNIV
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