Application of thiazolopyranone analogues in preparation of anti-liver fibrosis or anti-acute liver injury medicines

An anti-hepatic fibrosis and acute liver injury technology, applied in drug combination, digestive system, pharmaceutical formula, etc., can solve the problems of limited clinical application and low effective dose, and achieve a significant effect in the treatment of acute liver injury

Active Publication Date: 2019-04-26
LANZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Currently approved drugs for the treatment of fibrotic diseases include pirfenidone and nintedanib, but both are drugs specifically for the treatment of idiopathic pulmonary fibrosis (IPF). treatment has certain limitations
In addition, studies have shown that colchicine can achieve the effect of treating liver cirrhosis and liver fibrosis through vari

Method used

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  • Application of thiazolopyranone analogues in preparation of anti-liver fibrosis or anti-acute liver injury medicines
  • Application of thiazolopyranone analogues in preparation of anti-liver fibrosis or anti-acute liver injury medicines
  • Application of thiazolopyranone analogues in preparation of anti-liver fibrosis or anti-acute liver injury medicines

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Experimental program
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Embodiment Construction

[0036] The synthesis and anti-hepatic fibrosis and anti-acute liver injury activities of the thiazolopyrone analogs of the present invention will be described in detail below in conjunction with specific examples. It should be understood that these examples illustrate the present invention, but do not limit the scope of the present invention.

[0037] The experimental data involved in the activity experiment of the present invention are expressed as mean ± standard deviation (Mean ± SD).

[0038] 1. Structure and synthesis of thiazolopyrone analogs

[0039] In Examples 1-23, the structures of thiazolopyrone analogues are as follows:

[0040]

[0041] According to different configurations, the synthesis method of the above-mentioned chiral thiazolopyrone analogs can be selected, and according to different compounds, attention should be paid to the selection of the corresponding 5-enthiazolone substrate during the synthesis process. In Examples 1-23, the configurations and ...

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Abstract

The invention provides new medical application of thiazolopyranone analogues, in particular relates to application of the thiazolopyranone analogues in preparation of anti-liver fibrosis or anti-acuteliver injury medicines. A general structural formula of the thiazolopyranone analogues is described in the description; classical pharmacology experiments confirm that the thiazolopyranone analoguescan down-regulate the expression of a smooth muscle actin alpha-SMA and a transforming growth factor (TGF)-beta 1 in human hepatic stellate cells LX-2, thereby inhibiting the proliferation and transformation of the human hepatic stellate cells LX-2. In a model experiment of CCl4-induced liver fibrosis/acute liver injury in mice, the thiazolopyranone analogues can inhibit the up-regulation of ALT and AST in the serum of the mice, and can inhibit the expression of the alpha-SMA and the TGF-beta 1 which are related to liver fibrosis; the analysis of various pathological sections and immunohistochemistry experiments also confirm that the analogues can effectively treat acute liver injury and liver fibrosis in the mice. Therefore, the thiazolopyranone compounds can be used as active substancesfor the preparation of the anti-liver fibrosis or anti-acute liver injury medicines.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry and relates to the application of thiazolopyrone analogs in the preparation of anti-hepatic fibrosis or anti-acute liver injury drugs. Background technique [0002] The liver is an important organ in the human body that mainly performs metabolic functions. It has the functions of deoxidation, metabolism, storage of glycogen, and secretory protein synthesis. A variety of reasons can lead to abnormal liver function. Acute liver injury is the basis of liver failure, and severe or persistent liver injury will eventually lead to liver failure. There are many causes of acute liver injury, including viral infection, improper medication, food additives, excessive intake and exposure to ethanol, ingestion of toxic food, radiation damage, etc. Due to complex reasons, there is no particularly effective drug for acute liver injury. Hepatic fibrosis is the response of the liver to chronic long-te...

Claims

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Application Information

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IPC IPC(8): A61K31/429A61P1/16
CPCA61P1/16A61K31/429
Inventor 王锐林利张旭刘慧云
Owner LANZHOU UNIVERSITY
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