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Application of 1,3-benzoxazolethiol-2-one compounds in preparing monoamine oxidase inhibitor

A kind of technology of benzoxanethiol and ketone compounds, applied in the field of medicine, can solve problems such as substrate selectivity difference

Inactive Publication Date: 2018-08-10
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, their selectivity to substrates is quite different

Method used

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  • Application of 1,3-benzoxazolethiol-2-one compounds in preparing monoamine oxidase inhibitor
  • Application of 1,3-benzoxazolethiol-2-one compounds in preparing monoamine oxidase inhibitor
  • Application of 1,3-benzoxazolethiol-2-one compounds in preparing monoamine oxidase inhibitor

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1: the test of compound of the present invention to monoamine oxidase inhibitor activity

[0018] 1. Experimental reagents

[0019] 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)

[0020] 2. Experimental method

[0021] 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%.

[0022] 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 an application of 1,3-benzoxazolethiol-2-one compounds, which are shown as Formula (I), in preparing a monoamine oxidase inhibitor. Based upon in-vitro enzymatic activity experimental tests, it is indicated that the compounds have good inhibitory activity on both monoamine oxidase A and monoamine oxidase B; therefore, a reference and a new thought are provided and developedfor the development of the novel MAO inhibitor (monoamine oxidase inhibitor) (shown as the Description).

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a new pharmaceutical application of a 1,3-benzoxathiol-2-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 the express...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/39A61P25/24A61P25/04A61P25/06A61P25/16A61P25/00
CPCA61K31/39A61P25/00A61P25/04A61P25/06A61P25/16A61P25/24
Inventor 孔德信王栋左之利王雅琪
Owner HUAZHONG AGRI UNIV
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