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Antifungal compound and application thereof

A compound and antifungal technology, applied in the field of compounds, can solve the problems of poor patient tolerance, many adverse reactions, long half-life, etc., and achieve the effect of excellent broad-spectrum antifungal activity and strong inhibitory effect

Pending Publication Date: 2019-12-13
赵洁
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, in the application of clinical antifungal drugs, drug resistance, long half-life, many adverse reactions, poor tolerance of patients, etc. are prone to occur. Therefore, it is necessary to provide more new antifungal drugs that can solve one or more of the above shortcomings.

Method used

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  • Antifungal compound and application thereof
  • Antifungal compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1 prepares compound

[0018]

[0019] Put compound 1 (500mg) in a 50mL dry two-necked bottle, under nitrogen protection, add 10mL of anhydrous DMF, drop 1mL of anhydrous pyridine at 0°C at 1mL / min, and then dropwise add 3-chloro -4-trifluoromethyl-benzoyl (400mg), react at room temperature for 2-4 hours, add water to quench the reaction, extract with dichloromethane (20×3), and wash the organic phase 3 times with saturated brine, without Dry over sodium sulfate, filter, collect the filtrate and concentrate under reduced pressure, perform column chromatography, the eluent is chloroform:methanol (V:V) = 30:1, and compound 2 is obtained as a colorless viscous liquid.

[0020] Compound 2 (250 mg) was placed in a single-port reaction flask, dissolved in 50 mL of methanol, 100 mg of 10% Pd / C was added, vacuumed, and the reaction system was reacted overnight at room temperature under the protection of hydrogen; after the reaction was completed, the reaction solut...

Embodiment 2

[0024] Embodiment 2 (antifungal activity test)

[0025] 1. Experimental strain: Candida albicans (CMCC98001).

[0026] 2. Culture medium: Sabouraud medium was used for Candida albicans.

[0027] The specific formula of the medium is as follows: Sabouraud medium: peptone 10g, glucose 40g, add water to make 1 liter solution.

[0028] 3. Preparation of bacterial suspension:

[0029] The strains are stored on a slant semi-solid medium to maintain the purification and activity of the colony (preserved in a refrigerator at 4°C). When in use, the colonies are inoculated in the liquid medium, cultured on a shaker at 27°C for 24-48 hours, and the concentration of the bacterial suspension is controlled between 1-5×108 / ml with a hemocytometer.

[0030] 4. Preparation of antibacterial compounds:

[0031] compound They were numbered as compounds a, b, and c in sequence. Compounds a, b, and c were dissolved in (dimethyl sulfoxide) DMSO, prepared to 10 mg / ml, filtered through a 0.2 μm...

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PUM

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Abstract

The invention provides an antifungal compound, and a preparation method and application thereof. The compound has excellent broad-spectrum antifungal activity and strong inhibition effect on common fungi such as Saccharomyces cerevisiae, Aspergillus nidulans and Penicillium marneffei, especially on the important medical fungus--Candida albicans; and the antifungal compound can be used for treatingor preventing infectious diseases caused by fungi and thus has good clinical application prospects.

Description

technical field [0001] The present invention relates to a compound, in particular to an antifungal compound, and also relates to a preparation method and application of the antifungal compound. Background technique [0002] Fungi are eukaryotic microorganisms that exist widely in nature. So far, more than 200 kinds of fungi have been found to cause human diseases or harm animals and plants (such as blast fungi that harm rice, etc.). Human diseases caused by fungi are divided into superficial infections and deep infections. Superficial fungal infections are mainly caused by Epidermophyton, Microsporum, and Trichophyton, manifested as tinea capitis, tinea corporis, tinea versicolor, and onychomycosis. The main pathogens of deep mycoses include Candida, Cryptococcus, Aspergillus, Sporotrichum, etc., which mainly infect the digestive tract and respiratory system, which are extremely harmful and have a high fatality rate. With the wide application of high-efficiency broad-spec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/69C07D213/68A61K31/4412A61P31/10
CPCC07D213/69C07D213/68A61P31/10
Inventor 赵洁杨阳吕冰洁
Owner 赵洁
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