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Application of acetylcholin esterase inhibitor in preparation of medicine for treating Alzheimer's disease and preparation method of acetylcholin esterase inhibitor

A technology of inhibitors and drugs, applied in the direction of pharmaceutical formulations, drug combinations, nervous system diseases, etc., can solve problems such as limited options and achieve good inhibitory effect

Active Publication Date: 2021-11-05
SHANDONG FIRST MEDICAL UNIV & SHANDONG ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Therefore, the existing AD treatment drugs have great limitations in selection. After a certain drug is taken for a long time to produce cumulative side effects or resistance, the patient can improve the drug treatment plan Choices are limited

Method used

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  • Application of acetylcholin esterase inhibitor in preparation of medicine for treating Alzheimer's disease and preparation method of acetylcholin esterase inhibitor
  • Application of acetylcholin esterase inhibitor in preparation of medicine for treating Alzheimer's disease and preparation method of acetylcholin esterase inhibitor
  • Application of acetylcholin esterase inhibitor in preparation of medicine for treating Alzheimer's disease and preparation method of acetylcholin esterase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Preparation of 3-((3,5-dimethoxybenzyl)amino)-8-methoxycoumarin (referred to as compound I in the following examples)

[0031]

[0032] Reagents and conditions: (a) methanol, 50°C; (b) concHCl, methanol; (c) potassium carbonate, N,N-dimethylformamide, 102°C.

[0033] Synthetic method of intermediate 3-aminocoumarin: Synthesis of intermediate 3-formamido-8- Methoxycoumarin. Under the condition of magnetic stirring, first add 2-hydroxy-3-methoxybenzoic acid to the methanol solution, then add ethyl isocyanoacetate and pyridine, and finally add cuprous iodide, and put the reaction mixture in a 50°C oil bath Stir and heat in the pot for 6 hours, and monitor the progress of the reaction by TLC. After the reaction, the crude solid compound was obtained by filtration, washed three times with methanol solution, 15 ml each time, and the yield of light yellow solid 3-formamidocoumarin was 85%. Reflux 8-methoxy-3-formamidocoumarin with concentrated hydrochloric acid...

Embodiment 2

[0035] Embodiment 2 pharmacological activity experiment

[0036] Determination of 3-((3,5-dimethoxybenzyl)amino)-8-methoxycoumarin in vitro acetylcholinesterase inhibitory activity:

[0037] 1. Preparation of reaction solution

[0038](1) Preparation of PBS buffer solution: Accurately weigh 71.63g of disodium hydrogen phosphate, add an appropriate amount of distilled water to dissolve, then use a volumetric flask to accurately adjust the volume to 1L, and prepare a 0.2mol / L disodium hydrogen phosphate solution; accurately weigh 31.20 g sodium dihydrogen phosphate, add appropriate amount of distilled water to dissolve, then use a volumetric flask to accurately adjust the volume to 1L, and prepare a 0.2mol / L sodium dihydrogen phosphate solution. Accurately measure 473.50mL disodium hydrogen phosphate solution and 26.50mL sodium dihydrogen phosphate solution, mix them, add distilled water and use a volumetric flask to accurately adjust the volume to 1L, and prepare 0.1mol / L, PH=...

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Abstract

The invention relates to a medicine for treating Alzheimer's disease, and belongs to the field of chemical medicines. The invention provides an acetylcholin esterase inhibitor which is used for preparing a medicine for treating Alzheimer's disease. The compound has the activity of relieving the Alzheimer's disease, plays a role in various ways of inhibiting acetylcholin esterase and monoamine oxidase B, resisting oxidation activity and the like, and can be used as a multi-target medicine for treating the Alzheimer's disease.

Description

technical field [0001] The invention relates to the application of an acetylcholinesterase inhibitor in the preparation of medicine for treating Alzheimer's disease. Background technique [0002] Alzheimer's disease (AD), also known as senile dementia, is a degenerative disease of the central nervous system with an insidious onset and a chronic progressive course. It is the most common type of senile dementia. The main manifestations are neuropsychiatric symptoms such as progressive memory impairment, cognitive dysfunction, personality changes, and language barriers, which seriously affect social, occupational, and life functions. The characteristic pathological changes of AD are extracellular senile plaques formed by the deposition of β-amyloid protein, neurofibrillary tangles formed by hyperphosphorylation of tau protein, and neuron loss with glial cell proliferation. With the aging population in my country, the prevalence of AD is increasing year by year. According to st...

Claims

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Application Information

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IPC IPC(8): A61K31/352C07D311/12A61P25/28
CPCA61K31/352C07D311/12A61P25/28
Inventor 孙捷潘银波王晓静刘腾孙小雅郝灿华
Owner SHANDONG FIRST MEDICAL UNIV & SHANDONG ACADEMY OF MEDICAL SCI
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