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Application of (N-isopropylpiperazine)-2-hydroxybenzamide compound to preparation of drugs for treating neurodegenerative disease

A technology of hydroxybenzamide and isopropylpiperazine, which is applied in the field of medicine, can solve problems such as memory loss and memory loss, and achieve strong antioxidant activity, low toxicity, and obvious neuroprotective effects

Inactive Publication Date: 2017-06-06
NANYANG NORMAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the above-mentioned patents mainly focus on the research on nerve cell damage caused by oxidative stress. Oxidative stress is an intermediate link in the development of AD, which may be caused by factors such as excessive metal ion disorder or β-amyloid deposition. AD patients Excessive metal ions are found in the brain, and the disorder of metal ions is also a factor leading to AD. Studies have shown that the lack of acetylcholine levels in the brain of AD patients is the main cause of memory loss in AD patients. The enzymes that hydrolyze acetylcholine mainly include acetylcholinesterase and acetylcholine. Acylcholinesterase
With the development of the process of AD, the level of acetylcholinesterase (AChE) gradually decreases, while the activity of butyrylcholinesterase (BuChE) increases to 165% of the normal value, and the above-mentioned patent has no inhibitory activity to butyrylcholine

Method used

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  • Application of (N-isopropylpiperazine)-2-hydroxybenzamide compound to preparation of drugs for treating neurodegenerative disease
  • Application of (N-isopropylpiperazine)-2-hydroxybenzamide compound to preparation of drugs for treating neurodegenerative disease
  • Application of (N-isopropylpiperazine)-2-hydroxybenzamide compound to preparation of drugs for treating neurodegenerative disease

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Embodiment 1

[0033] A use of (N-isopropylpiperazinyl)-2-hydroxybenzamide compound in the preparation of medicines for treating neurodegenerative diseases, the chemical structural formula of the compound is:

[0034]

[0035]The preparation method of above-mentioned (N-isopropylpiperazinyl)-2-hydroxybenzamide compound comprises the following steps:

[0036] Add 0.724mol salicylic acid (1), EDCI, HOBT and 4mL anhydrous dichloromethane into a 10mL round bottom flask, stir at room temperature for 30min, then add 0.483mol isopropylpiperazine (2) (compound (1) and (2) The molar ratio is 1.5:1), TLC detects the reaction, reacts at room temperature for 15h, after the reaction finishes, adds 30mL dichloromethane to the reaction solution, washes with saturated NaHCO 3 Wash with aqueous solution (20mL×3), then wash with 20mL of saturated sodium chloride solution, dry the organic layer with anhydrous sodium sulfate, filter, and evaporate the solvent to dryness under reduced pressure. The obtained c...

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to application of an (N-isopropylpiperazine)-2-hydroxybenzamide compound to preparation of drugs for treating neurodegenerative disease, especially the application of preparation of drugs for treating Alzheimer's disease. The chemical structural formula of a salicylate compound is shown as the formula I. The (N-isopropylpiperazine)-2-hydroxybenzamide compound provided by the invention has butyrylcholine esterase inhibiting activity, antioxidant activity and metal ion coordination activity, has an obvious neuroprotection effect on hydrogen peroxide induced PC12 cellular damage, further shows a better effect in treating Alzheimer's disease in experiments in vivo, is relatively low in toxicity and has good clinical prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the use of a (N-isopropylpiperazinyl)-2-hydroxybenzamide compound in the preparation of drugs for neurodegenerative diseases, especially in the preparation of drugs for Alzheimer's disease use in . 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 in the world suffered from dementia in 2015. It is predicted th...

Claims

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Application Information

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IPC IPC(8): A61K31/495A61P25/28
CPCA61K31/495
Inventor 桑志培柳文敏王柯人潘万里马勤阁于林涛毛武涛蔡贤淑
Owner NANYANG NORMAL UNIV
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