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Use of a 5h-thiazolo[3,2-a]pyrimidin-5-one compound in the preparation of monoamine oxidase inhibitors

A kind of technology of monoamine oxidase and ketone compounds, applied in the field of medicine

Active Publication Date: 2021-05-04
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 5H-thiazolo[3,2-a]pyrimidin-5-one derivatives have potential biological activities as purine structural analogues. However, there is no report on its use as a monoamine oxidase inhibitor

Method used

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  • Use of a 5h-thiazolo[3,2-a]pyrimidin-5-one compound in the preparation of monoamine oxidase inhibitors
  • Use of a 5h-thiazolo[3,2-a]pyrimidin-5-one compound in the preparation of monoamine oxidase inhibitors
  • Use of a 5h-thiazolo[3,2-a]pyrimidin-5-one compound in the preparation of monoamine oxidase inhibitors

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Embodiment 1

[0021] Embodiment 1: the test of compound of the present invention to monoamine oxidase inhibitor activity

[0022] 1. Experimental reagents

[0023] Compounds of the present invention, MAOA (Active Motif, Cat.No.31502), MAOB (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)

[0024] 2. Experimental method

[0025] 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%.

[0026] 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 measure...

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Abstract

The invention discloses the use of 5H-thiazolo[3,2-a]pyrimidin-5-one compounds with the structure shown in formula (I) in the preparation of monoamine oxidase inhibitors. After in vitro enzyme activity test, the compounds It has good inhibitory activity on monoamine oxidase A and B, which provides reference and inspires new ideas for the development of new MAO inhibitors.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a new pharmaceutical application of a 5H-thiazolo[3,2-a]pyrimidin-5-one compound, especially a new application in preparing 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 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519A61P25/24A61P25/28A61P25/00A61P25/06A61P25/18
CPCA61K31/519A61P25/00A61P25/06A61P25/18A61P25/24A61P25/28
Inventor 孔德信王栋
Owner HUAZHONG AGRI UNIV
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