Applications of 1-tetralone compound in preparation of monoamine oxidase inhibitors

Inactive Publication Date: 2020-11-10
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 1-tetralone is an important chemical intermediate, mainly used in dehydrogenation of methylnaphthol; the pharmaceutical industry is used to synthesize 18-methyl norethindrone (contraceptive), rodenticide, and also to synthesize benzo It is an important intermediate of Puli (hypertensive drug). In addition, it can also be used as a softener for solvents and plastics. Its chloride has insecticidal effects. There is no literature report that 1-tetralone is used to inhibit monoamine oxidase

Method used

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  • Applications of 1-tetralone compound in preparation of monoamine oxidase inhibitors
  • Applications of 1-tetralone compound in preparation of monoamine oxidase inhibitors
  • Applications of 1-tetralone compound in preparation of monoamine oxidase inhibitors

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Experimental program
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Embodiment 1

[0026] Embodiment 1: the test of compound of the present invention to monoamine oxidase inhibitor activity

[0027] 1. Experimental reagents

[0028] Compounds of the present invention, MAO-A (Active Motif, Cat.No.31502), MAO-B (Active Motif, Cat.No.31503), Clogyline (Sigma, Cat.No.M3778), srigiline R (-)-deprenyl (Abcam, Cat.No.ab120604), 384-well plate (from Perkin Elmer, Cat.No.6007299)

[0029] 2. Experimental method

[0030] 1) Dissolve the compound of the present invention to 100 mM with 100% DMSO, add HEPES buffer in the multi-well plate, transfer the compound to the multi-well plate, and reduce the concentration of DMSO to 1%.

[0031] 2) Dissolve the enzyme and the substrate into the buffer solution respectively, transfer 10 μL of the substrate solution, start the reaction, let stand for 60 minutes, add 20 μL of luciferin, mix well, stand at room temperature for 20 minutes, measure and record the fluorescence signal The relative brightness of the compound was measu...

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Abstract

The invention discloses applications of 1-tetralone compound in preparation of monoamine oxidase inhibitors. The structure of the compound is shown as a formula (I). Through enzyme activity test in vitro, the compound can have good inhibitory activity on monoamine oxidase A and B, so that reference and new inspiring ideas can be provided for the development of novel MAO inhibitors.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a new pharmaceutical application of a 1-tetralone compound, especially a new application in the preparation of monoamine oxidase inhibitors. Background technique [0002] Monoamine neurotransmitters include norepinephrine, epinephrine, dopamine, and serotonin, and are the most important class of neurotransmitters. The expression levels of these neurotransmitters and their metabolites are closely related to many diseases, affecting human attention, emotion and behavior. For example, a decrease in the concentration of 5-HT in the human body can cause depression; a decrease in the concentration of dopamine in the nervous system can induce Parkinson's syndrome and Alzheimer's disease. The degradation regulation of these monoamine neurotransmitters is mainly accomplished by monoamine oxidase (monoamine oxidase, MAO). Therefore, inhibiting the activity of MAO can increase the expressio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61K31/135A61P25/28A61P25/16A61P25/24A61P25/04A61P25/02A61P29/00A61P25/00
CPCA61K31/122A61K31/135A61P25/00A61P25/02A61P25/04A61P25/16A61P25/24A61P25/28A61P29/00
Inventor 孔德信王栋
Owner HUAZHONG AGRI UNIV
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