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Synthetic method of petrosiols A-E and pharmaceutical potential thereof

A technology for drugs and compounds, applied in the field of chemistry and medicine, can solve the problems of low penetration of the blood-brain barrier and limited wide application.

Inactive Publication Date: 2019-06-21
RES CENT FOR ECO ENVIRONMENTAL SCI THE CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nerve growth factor NGF (Nerve growth factor) is considered to be an effective drug for the treatment of neurodegenerative diseases, but its wide application is limited due to its large molecular weight and excellent hydrophilicity leading to low penetration of the blood-brain barrier.

Method used

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  • Synthetic method of petrosiols A-E and pharmaceutical potential thereof
  • Synthetic method of petrosiols A-E and pharmaceutical potential thereof
  • Synthetic method of petrosiols A-E and pharmaceutical potential thereof

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Experimental program
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Embodiment Construction

[0024] 1. All biological experiments are operated according to standardized and known procedures. Experimental model mice are purchased and raised from qualified animal rooms. All relevant parameters are completed in the Toxicology Laboratory of the Eco-Environmental Research Center of the Chinese Academy of Sciences. .

[0025] 2. The idea of ​​divergent synthesis is as shown in formula 1. The synthesis of Petrosiol E is taken as an example below to specifically illustrate the new method for preparing the compound. Other Petrosiols compounds can be completed by personnel with professional knowledge with reference to the method disclosed in the present invention.

[0026]

[0027] 1. Provide the following examples of the present invention (taking the above compound Petrosiol E as an example):

[0028] Synthesis of Compound 18:

[0029] 0°C, under nitrogen protection, dissolve 10-bromodecyl alcohol (1eqv) and catalytic amount of cuprous chloride in dry tetrahydrofuran, add ...

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Abstract

The invention discloses potential of compounds petrosiols A-E in the treatment of Alzheimer's disease and Parkinson's disease. Through a model mouse, the effects of object compounds in relieving Alzheimer's disease and Parkinson's disease are studied respectively. Main investigations are provided for the compounds' improvement on behavioristics of the disease model mouse, the change in the dopamine content of the model mouse fed with the compounds, the influence on the quantity of neurons after the model mouse fed with the compounds, and the change in experimental other related parameters or factor. The results show that the compounds petrosiols A-E have the potential to treat Alzheimer's disease and Parkinson's disease. A divergent synthetic route of the compounds petrosiols A-E is designed herein, which has the main characteristics shown in the description.

Description

technical field [0001] The invention relates to a preparation method of Petrosiols A-E and its potential as medicine, belonging to the technical field of chemistry and medicine. Background technique [0002] Alzheimer's disease and Parkinson's syndrome are common neurodegenerative diseases. Neurodegenerative disease is a disease in which cells and neurons of the brain and spinal cord are lost. Normally, cells in the brain and spinal cord are generally unable to regenerate, and excessive damage can be devastating and irreversible. [0003] Studies on the pathological mechanism of such diseases have shown that neuron damage and oxidative stress are the main reasons for the development of neurodegenerative diseases. Therefore, the ability to effectively improve oxidative stress, promote neuronal differentiation and reduce cell death is considered to be an effective way to effectively treat neurodegenerative diseases. Nerve growth factor NGF (Nerve growth factor) is considere...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/047A61P25/16A61P25/28C07C29/36C07C33/04C07C33/048
Inventor 杜宇国耿佳琳刘思金
Owner RES CENT FOR ECO ENVIRONMENTAL SCI THE CHINESE ACAD OF SCI