Bromine-containing compounds as antifungal agents

A technology of antibacterial drugs and compounds, applied in the field of bromine-containing compounds, can solve the problems of large dosage and frequent use, and achieve the effect of small MIC value and excellent antifungal effect

Pending Publication Date: 2021-06-04
BEIJING TECHNOLOGY AND BUSINESS UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, antifungal drugs mainly include allylamine, triazole, imidazole, echinocandin, and flucytosine, but fungal drug resistance is becoming more and more serious. more frequent and larger doses of drugs needed to treat fungal infections

Method used

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  • Bromine-containing compounds as antifungal agents
  • Bromine-containing compounds as antifungal agents
  • Bromine-containing compounds as antifungal agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1, the synthesis of compound I1N-(4-bromophenylthiazol-2-yl)acetone hydrazone (N-(4-bromophenyl-2-thiazolyl)acetone hydrazone)

[0027] The synthetic route is as follows:

[0028]

Embodiment 2

[0031] Separation and purification of N-(4-bromophenylthiazol-2-yl)acetone hydrazone

[0032] The suspension after the reaction in Example 1 was used to filter using a Buchner funnel, fully washed with petroleum ether, and dried in vacuum. The dried solid powder was separated by forward silica gel column chromatography (forward silica gel 200-300 mesh, or 100-200 mesh), and eluted with a mixed solvent of petroleum ether and ethyl acetate (volume ratio: 3:1). The eluent containing compound I was dried under reduced pressure to remove the organic solvent to obtain the target compound.

Embodiment 3

[0033] The structure identification of embodiment 3 compound I1

[0034] HPLC was used to identify the purity of the prepared compound, and the samples with a purity greater than 98% were tested for structural identification by mass spectrometry and nuclear magnetic resonance technology, and the nuclear magnetic resonance was determined by a Bruker AVANCE DRX-500 nuclear magnetic resonance instrument; the mass spectrometer was determined by an Agilent 1946D single quadrupole mass spectrometer Determination.

[0035] The H NMR spectrum data of the target compound δ H (CDCl 3 ): 8.54(s), 7.64(d, J=8.5Hz), 7.49(d, J=8.5Hz), 6.84(s), 2.05(s), 1.84(s);

[0036] The carbon NMR spectrum data of the target compound δ H (CDCl 3 ): 169.7, 149.8, 149.5, 133.7, 131.9, 127.6, 121.8, 103.8, 25.2, 16.7;

[0037] ESI mass spectrum [M+H] of the target compound + m / z 310.0

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PUM

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Abstract

The invention discloses a bromine-containing compound as an antifungal drug. The invention claims to protect a compound as shown in a formula I or pharmaceutically acceptable salt, ester and solvate thereof. In the formula I, R is -NH2 or -N = C(CH3)2. The compound as shown in the formula I provided by the invention has a more excellent antifungal effect.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a bromine-containing compound as an antifungal medicine. Background technique [0002] At present, antifungal drugs mainly include allylamine, triazole, imidazole, echinocandin, and flucytosine, but fungal drug resistance is becoming more and more serious. More and more frequently, the doses of drugs required to treat fungal infections are also increasing. Fungal infection is a serious threat to human health, so it is necessary to develop new drugs for the treatment of fungal infections. Contents of the invention [0003] The object of the present invention is to provide a bromine-containing compound as an antifungal drug. [0004] The present invention claims to protect the compound represented by formula I or its pharmaceutically acceptable salt, ester, solvate, [0005] [0006] In the formula I, R is -NH 2 or -N=C(CH 3 ) 2 . [0007] In the compound represented by the above f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/50A61K31/426A61P31/10
CPCC07D277/50A61P31/10
Inventor 宋福行毕洪凯贾佳杜冠华王守宝杨娜李红花艾娜丝
Owner BEIJING TECHNOLOGY AND BUSINESS UNIVERSITY
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