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Application of N-(thiazole-2-yl)-3-(piperazine-1-yl)propionamide compound in preparation of medicines

A compound, propionamide technology, applied in the field of medicine, can solve problems such as no treatment means

Active Publication Date: 2019-03-01
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is currently no clinically effective treatment

Method used

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  • Application of N-(thiazole-2-yl)-3-(piperazine-1-yl)propionamide compound in preparation of medicines
  • Application of N-(thiazole-2-yl)-3-(piperazine-1-yl)propionamide compound in preparation of medicines
  • Application of N-(thiazole-2-yl)-3-(piperazine-1-yl)propionamide compound in preparation of medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 The dose-effect relationship of the active compound inhibiting the release of inflammatory factors from macrophages stimulated by LPS

[0027] In order to test the dose-effect relationship of active compounds inhibiting the release of IL-6 from RAW 264.7 macrophages stimulated by LPS. The specific method is as follows: 1.2×10 6 Primary macrophages were cultured with DMEM medium at 37°C. After 24 hours, the medium was renewed, and the test compound (final concentration: 10 μM) was added for pretreatment for 2 hours, and then treated with 0.5 μg / mL LPS for 22 hours. , collect the culture fluid and use the ELISA method to detect the IL-6 content; collect the cells to detect the total protein concentration, and the ELISA results are divided by the corresponding total protein concentration for calibration. The IL-6 content of the LPS control group is calibrated as 100, and the average value is calculated and error value. See the experimental results figure 1 . ...

Embodiment 2

[0028] Compound of Example 2 alleviates physiological changes in rats with acute lung injury

[0029] Suspensions were prepared with 0.5% sodium carboxymethylcellulose and compounds LM8 and LM9 for intraperitoneal administration. Rats in each group were exposed to the trachea after ether anesthesia. Except for the control group, 50 μL 5 mg / kg LPS was slowly instilled into the trachea of ​​the other groups to cause acute lung injury in the rats. Wounds were used to establish an acute lung injury model. After 24 hours of animal modeling, mice were anesthetized by intraperitoneal injection of 10% chloral hydrate at a dose of 5 mL / kg, the left lung was ligated by thoracotomy, and bronchoalveolar lavage was performed on the right lung with 1 mL of normal saline, and the lavage fluid was collected. The same operation was repeated for 3 Second-rate.

[0030] After the alveolar lavage fluid was collected, it was centrifuged at 1000 rpm at 4°C for 5 minutes, and the supernatant was t...

Embodiment 3

[0032] Example 3 compound alleviates the pathological change test of lung tissue in acute lung injury

[0033] For experimental data, see image 3 , the alveolar cavity of rats in the normal control group was clear, the structure was complete, and the wall was smooth; after the acute lung injury model was induced by tracheal instillation of LPS, the alveolar wall was obviously edematized and thickened, and the infiltration of inflammatory cells increased; after treatment with compounds LM8 and LM9, the cells edema, The thickening was significantly weakened, and the infiltration of inflammatory cells was significantly reduced, which was not much different from the normal group, indicating that the compound can effectively relieve lung tissue damage in acute lung injury.

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Abstract

The invention discloses an application of a N-(thiazole-2-yl)-3-(piperazine-1-yl)propionamide compound in preparation of medicines. The compound is used for preparing an anti-inflammation medicine; test results prove that the compound has anti-inflammation activity, especially treating acute lung injury due to over-expression and over-release of TNF-alpha and / or IL-6.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the use of a compound of formula (I) (code LM9) or a pharmaceutically acceptable salt thereof in the preparation of medicines for treating or preventing inflammatory diseases. [0002] Background technique [0003] As an important pathological process, inflammation is an autoimmune response of the human body to external or foreign stimuli. And when this response is dysregulated or overreacted, causing the body to self-injury, it gradually evolves into inflammation. In the process of inflammation, inflammatory factors will directly or indirectly cause tissue and cell damage. [0004] Acute Lung Inflammation (ALI) is the injury of alveolar epithelial cells and capillary endothelial cells caused by various indirect or direct injury factors, resulting in diffuse pulmonary interstitial and alveolar edema, leading to acute hypoxic respiratory insufficiency . The death...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61P29/00A61P11/00
CPCA61K31/496A61P11/00A61P29/00
Inventor 梁广陈凌峰张亚利蔡跃飘
Owner WENZHOU MEDICAL UNIV
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