Flavonoid derivative as well as preparation method, pharmaceutical composition and application thereof

By modifying flavonoids and introducing lipophilic groups, the problem of insufficient blood-brain barrier ability is solved, and the effect of increasing the concentration of drugs in the brain and retaining antioxidant and anti-inflammatory functions is achieved, and the effect of neuroprotection and anesthesia is improved.

CN119751232AActive Publication Date: 2025-04-04SHENZHEN PEOPLES HOSPITAL
4 Cites 0 Cited by

Patent Information

Application Number
CN202411645425.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-11-18
Publication Date
2025-04-04
Estimated Expiration
2044-11-18

AI Technical Summary

Technical Problem

Due to poor fat solubility and insufficient ability to pass through the blood-brain barrier, existing flavonoids have low bioavailability in the brain and are unable to effectively exert antioxidant, anti-inflammatory and neuroprotection functions.

Method used

By introducing lipophilic groups and performing structural modifications similar to propofol based on the skeleton structure, novel flavonoid derivatives have been developed to enhance their lipid solubility to improve their ability to pass through the blood-brain barrier.

Benefits of technology

It increases the concentration of drugs in the brain of flavonoid derivatives, maintains the level of pharmacokinetics, retains antioxidant, anti-inflammatory and nerve regeneration functions, reduces nerve cell damage, enhances anesthesia, and has potential antidepressant effects.

✦ Generated by Eureka AI based on patent content.
Patent Text Reader

Abstract

The invention relates to the field of medical chemistry, and discloses a flavonoid derivative as well as a preparation method, a pharmaceutical composition and application thereof. The general structural formula of the flavonoid derivative is # imgabs0 #, wherein R2 and R '2 are independently selected from-H,-OH or-OCH3; r3 and R '3 are independently selected from-H,-CH3,-OCH3,-CH (CH3) 2 or-CH (CH2) 2; r5 and R '5 are independently selected from-H,-CH3,-OCH3,-CH (CH3) 2 or-CH (CH2) 2; and R6 and R '6 are independently selected from-H,-OH or-OCH3. The flavonoid derivative is enhanced in fat solubility, is beneficial to penetrating through BBB, improving the concentration of drugs in the brain and maintaining the pharmacokinetic level, effectively retains the neuroprotective effects of oxidative stress resistance, inflammation resistance, nerve regeneration and the like, propofol is introduced into a flavonoid skeleton, the anesthetic effect is enhanced under the synergistic effect of propofol and propofol, and the flavonoid derivative can become a potential new anti-depression drug.
Need to check novelty before this filing date? Find Prior Art