Pterostilbene chalcone compounds, their preparation methods and medical uses

By synthesizing pterostilbene chalcone compounds, the limitations of pterostilbene and paeonol in clinical applications were resolved, and a potent anti-inflammatory effect was achieved, which is suitable for the development of new anti-inflammatory drugs.

CN118388430BActive Publication Date: 2025-09-19ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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Patent Information

Application Number
CN202410426021.3
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2024-04-10
Publication Date
2025-09-19
Estimated Expiration
2044-04-10

AI Technical Summary

Technical Problem

The clinical application of pterostilbene and paeonol is limited due to their easy oxidation, low bioavailability and poor water solubility. Chalcone compounds have weak activity and it is difficult to achieve good anti-inflammatory effects.

Method used

Pterostilbene chalcone compounds were designed and synthesized. By combining pterostilbene with paeonol, a series of novel structural compounds were formed, which enhanced the anti-inflammatory activity and improved the physicochemical properties. The compounds were prepared by a multi-step reaction involving acid chlorides, alkaline reagents and solvents.

Benefits of technology

Pterostilbene chalcone compounds significantly inhibit the activity of key inflammatory mediators such as cyclooxygenase, inducible nitric oxide synthase and nuclear factor κB, have excellent anti-inflammatory effects, and their inhibitory effects are better than indomethacin, making them suitable for development as new anti-inflammatory drugs.

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Abstract

The present invention discloses a pterostilbene chalcone compound represented by general formula (I) or a pharmaceutically acceptable salt thereof. The compound has a strong inhibitory effect on LPS-induced NO production in RAW264.7 cells, significantly superior to indomethacin, and can be developed into a new anti-inflammatory drug. The preparation method of the compound of the present invention is characterized by readily available raw materials, simple operation, and high yield.
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