Use of a thiadiazolotriazine compound in the preparation of monoamine oxidase inhibitors

A monoamine oxidase and compound technology, applied in the field of medicine, can solve problems such as differences in substrate selectivity

Inactive Publication Date: 2020-08-28
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There is a high degree of similarity between the two isoforms, but there is a large difference in their substrate selectivity

Method used

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  • Use of a thiadiazolotriazine compound in the preparation of monoamine oxidase inhibitors
  • Use of a thiadiazolotriazine compound in the preparation of monoamine oxidase inhibitors

Examples

Experimental program
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Embodiment 1

[0015] Embodiment 1: the test of compound of the present invention to monoamine oxidase inhibitor activity

[0016] 1. Experimental reagents

[0017] 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)

[0018] 2. Experimental method

[0019] 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%.

[0020] 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 the application of a triazine compound shown as a structural formula (I) in the preparation of a monoamine oxidase inhibitor. Through in vitro enzyme activity experimental measurement, the compound has good inhibitory activity for monoamine oxidase-B, so that reference is provided for developing a novel MAO inhibitor, and a new thought is inspired.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a new pharmaceutical application of a thiadiazolotriazine 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 expression...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/53C07D513/04A61P25/28
CPCA61K31/53C07D513/04
Inventor 孔德信王栋左之利王雅琪
Owner HUAZHONG AGRI UNIV
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