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Exogenous hydrogen sulfide donor, and preparation and application thereof

A hydrogen sulfide donor, exogenous technology, applied in the field of medicine, can solve the problems of glutathione stimulation, anesthetic effect in the central nervous system, etc.

Inactive Publication Date: 2017-07-07
川北医学院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of hydrogen sulfide in the body undergoes oxidative metabolism to form thiosulfate and sulfate for detoxification. During the metabolic process, glutathione may play a stimulating role; a small part can be metabolized by methylation to form less toxic methyl mercaptan and formazan. Thioether, but high concentrations of methyl mercaptan have an anesthetic effect on the central nervous system

Method used

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  • Exogenous hydrogen sulfide donor, and preparation and application thereof
  • Exogenous hydrogen sulfide donor, and preparation and application thereof
  • Exogenous hydrogen sulfide donor, and preparation and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0035] An exogenous hydrogen sulfide donor with the following structure:

[0036]

Embodiment 2

[0038] The preparation method of compound I of the present invention comprises the following steps:

[0039] A, dissolving captopril in dichloromethane, adding acetyl chloride, then adjusting the pH value to 8-9, continuing the reaction to obtain an intermediate product;

[0040] B. Reacting the intermediate product with nortrithione in dichloromethane as a solvent to obtain compound I as the final product.

Embodiment 3

[0042] The preparation method of compound II of the present invention comprises the following steps:

[0043] A, proglumide is dissolved in the solvent dichloromethane, added successively nortrisulfide, DCC (dicyclohexylcarbodiimide), DMAP (4-dimethylaminopyridine), nitrogen protection reaction at room temperature;

[0044] B. After stopping the reaction, add NaOH solution dropwise to the reaction system until the pH value is 7, filter with suction, add water layer to the filtrate in a separatory funnel, add anhydrous sodium sulfate to the dichloromethane layer to remove residual water, spin Evaporated to dryness to obtain the final product.

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Abstract

The invention provides an exogenous hydrogen sulfide donor, and discloses a therapeutic action of an anethol trithione derivative used as the exogenous hydrogen sulfide donor on cardiovascular diseases. The exogenous hydrogen sulfide donor can release hydrogen sulfide, can promote the growth of an HUVEC (human umbilical vein endothelial cell) atherosclerosis cell model, has an antiatherosclerotic effect, and hopefully becomes a new target drug researched and developed by drugs with antiatherosclerotic effects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an exogenous hydrogen sulfide donor and its preparation and application. Background technique [0002] Hydrogen Sulfide (H 2 S) is a colorless toxic gas with the smell of rotten eggs. It is the third gas signal with a wide range of physiological activities found in the body after nitric oxide (NO) and carbon monoxide (CO). molecular. As a new type of gas signal molecule, hydrogen sulfide is widely involved in the regulation of various systems of the human body, especially in the human cardiovascular system. In recent years, many studies have been conducted on the pathogenesis of hydrogen sulfide in atherosclerosis in vitro and in vivo, and hydrogen sulfide has become a new direction in the research of atherosclerosis. [0003] Endogenous hydrogen sulfide is produced by the metabolism of sulfur-containing amino acids in mammals. Hydrogen sulfide is mainly produced...

Claims

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Application Information

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IPC IPC(8): C07D409/12C07D339/04A61K31/4025A61K31/381A61K33/04A61P9/10A61P9/00
CPCC07D409/12A61K31/381A61K31/4025A61K33/04C07D339/04
Inventor 周春阳陈钏李博袁斌欧学兰余刘勤梅雪杨春艳
Owner 川北医学院
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