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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
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  • 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

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  • 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.

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PUM

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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

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Application Information

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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
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