Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Baicalein derivative as well as preparation method and application thereof

A technology of baicalein and derivatives, which is applied in the field of medicine and can solve problems such as treatment failure of azoles

Active Publication Date: 2020-04-24
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
View PDF7 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, the resistance to the commonly used azole antifungal drugs, such as fluconazole, is becoming stronger and stronger, leading to the failure of the treatment of azoles

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Baicalein derivative as well as preparation method and application thereof
  • Baicalein derivative as well as preparation method and application thereof
  • Baicalein derivative as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0123] Embodiment 1: the preparation of compound S1

[0124]Put baicalein (BE) (500mg, 1.85mmol) in a 100ml single-necked bottle, add 30ml of MeOH to dissolve, then add formaldehyde (140μl, 2.78mmol) and diethylamine (300μl, 2.88mmol) successively, heat up to 40°C, and then The reaction was carried out under these conditions for 3 hours, and TLC detected that the reaction was complete. The solid was separated out by suction filtration, and then the filter cake was dried and placed in a 50 ml single-necked bottle and recrystallized with ethanol to obtain compound S1.

Embodiment 2

[0125] Example 2: Preparation of Compound S2 Refer to the preparation method of Compound S1, except that diethylamine is replaced by pyrrolidine.

Embodiment 3

[0126] Example 3: Preparation of Compound S3 Refer to the preparation method of Compound S1, except that diethylamine is replaced by morpholine.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a baicalein derivative, the structure of which is shown in the specification, in the formula, R1 is hydrogen, alkyl, or substituted / unsubstituted aryl; R2 is hydrogen, halogen,alkyl, alkoxy, substituted / unsubstituted amino, or substituted / unsubstituted aryl; R3 is oxygen or sulfur; and R4 is a substituted / unsubstituted aryl group. The synthesis method of the baicalein derivative is relatively simple and convenient; pollution is reduced, experiments prove that the prepared baicalein derivative can be used together with azole antifungal drugs, the sensitivity of drug-resistant bacteria to the azole drugs can be improved, that the drug resistance is reversed, and a novel way is provided for the treatment of drug-resistant fungi in clinic.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a baicalein derivative and its preparation method and application. Background technique [0002] In recent years, a large number of antibiotics and immunosuppressants have been used clinically, and the incidence of AIDS has increased year by year, and the incidence of fungal diseases is increasing. Moreover, the resistance to the commonly used azole antifungal drugs, such as fluconazole, is becoming stronger and stronger, resulting in the failure of the azole drugs. Therefore, finding new antifungal drugs, or antifungal drug resistance reversal agents, to improve the sensitivity of fungi to drugs, and to produce synergistic antifungal effects with existing drugs is an important method to improve the therapeutic effect of current existing drugs. [0003] Baicalein (Baicalein, BE), whose full name is 5,6,7-trihydroxybenzopyran-4-one, is a polyhydroxy flavone isolated ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/30C07D405/10A61K31/352A61K31/496A61K31/5377A61K31/453A61K31/40A61P31/10
CPCA61P31/10C07D311/30C07D405/10
Inventor 金永生董家潇高越王瀚萱倪廷峻弘李修政李伟姚淞允
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com