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Application of substituted piperazine compound in preparation of medicament for resisting fungal infection

A compound and antifungal technology, applied in the field of medicine, can solve problems such as poor metabolic properties and physical and chemical properties, poor bioavailability, inconvenient use by patients, etc., and achieve the effect of convenient source of raw materials, low cost and convenient source

Inactive Publication Date: 2013-04-03
DALI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the biggest problem facing echinocandycin is: there is no oral dosage form, only limited to injection (and limited to hospital use), so it is quite inconvenient for patients to use
Although the new product has an expanded antibacterial spectrum, it has poor metabolic properties and physical and chemical properties, low water solubility, and poor bioavailability; patients need a high-fat diet to facilitate drug absorption, or take expensive special preparations to take effect; in order to increase water solubility The added cyclodextrin also poses a greater threat to those with renal insufficiency

Method used

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  • Application of substituted piperazine compound in preparation of medicament for resisting fungal infection
  • Application of substituted piperazine compound in preparation of medicament for resisting fungal infection
  • Application of substituted piperazine compound in preparation of medicament for resisting fungal infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1: Preparation of (4-chlorophenyl)-(piperazin-1-yl)-methanone

[0018] 1.1 Instruments and reagents

[0019] The melting point was measured with a microscopic melting point apparatus (produced by Beijing Tektronix Co., Ltd.), and the temperature was not corrected; the optical rotation was measured on a Polax-2L automatic polarimeter made in Japan; the infrared spectrum IR was measured by a Bruker Vector-22 infrared spectrometer, and pressed by KBr; Spectra were measured with a Shimadzu UV-240 ultraviolet spectrophotometer; hydrogen nuclear magnetic resonance 1 H NMR, carbon nuclear magnetic resonance 13 C NMR and 2D NMR were measured by INOVA superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilyl ether TMS as internal standard); electrospray mass spectrometry ESI-MS was measured by Bruker Esquire 3000+ mass spectrometer, column layer Silica gel for analysis (100-200, 200-300 and 300-400 mesh) and silica gel GF254 for t...

Embodiment 2

[0025] Example 2: Antifungal activity test of compound of formula (1)

[0026] With reference to the standardized antifungal susceptibility test method proposed by the National Committee for Clinical Laboratory Standards (NCCLS), test the in vitro antifungal resistance of (4-chlorophenyl)-(piperazin-1-yl)-methanone prepared in Example 1. fungal activity.

[0027] 2.1 Fungal standard strain:

[0028] Candida albicans ATCC10231: Provided by Chongqing Center for Disease Control;

[0029] Candida albicans ATCC76615: Provided by Changzheng Hospital Affiliated to Second Military Medical University.

[0030] 2.2 Reagents:

[0031] 2.2.1 Sabouraud dextrose agar medium (sabouraud dextrose agar): product of Guangdong Kai Microbiology Technology Co., Ltd.

[0032] 2.2.2 Yeast extract: repackaged by Haishenggong Bioengineering Technology Service Co., Ltd.

[0033] 2.2.3 Three azamorphine propanesulfonic acid (3-N-morpholinopropanesulfonic acid, MOPS)

[0034] 2.2.4 Standard antifung...

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Abstract

The invention relates to the application of a substituted piperazine compound in the preparation of a medicament for resisting fungal infection and particularly discloses a compound which is (4-chlorophenyl)-(piperazin-1-yl)-methanone or pharmaceutically acceptable salt thereof as well as a preparation method and medicinal application of the (4-chlorophenyl)-(piperazin-1-yl)-methanone or medicinally acceptable salt thereof. The steps for synthesizing the compound are simple, the method for preparing the compound is simple and practical, the sources of raw materials are easy to obtain, the cost is low, and less pollution is caused. The compound has an obvious activity of inhibiting the growth of fungi and has the MIC value of 62.5mcg / ml. The pharmacodynamic results show that the substituted piperazine compound or medicinally acceptable salt is expected to be used to prepare the medicament for preventing and treating the diseases caused by fungal infection.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular, the invention relates to the use of piperazine compound (4-chlorophenyl)-(piperazin-1-yl)-methanone in the preparation of antifungal infection drugs. Background technique [0002] With the development of medical science, various new drugs and new technologies such as broad-spectrum antibiotics, hormones, various catheter intubation techniques, chemotherapy, transplantation and other medical methods are widely used, as well as HIV infection and tumors, causing the human immune system to be gradually The number of cases of destruction is increasing year by year, which leads to an increasing incidence of deep mycoses; on the other hand, with the widespread use of antibiotics and clinical antifungal drugs, traditional antibiotics cannot effectively fight against some serious fungal infections and Bacterial infections and fungal drug resistance are becoming more and more serious. The ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/495A61P31/10C07D295/192
Inventor 吴利先薛婷高鹏肖怀巫秀美赵昱钱金栿
Owner DALI UNIV
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