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Fluorobenzyl substituted piperazine compound and preparation and medical application thereof

A technology of fluorobenzyl compounds, which is applied in the field of preparation of antifungal infection drugs, can solve the problems of poor metabolic properties and physical and chemical properties, poor bioavailability, inconvenient use of patients, etc., and achieve convenient source of raw materials, low cost and convenient source Effect

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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  • Fluorobenzyl substituted piperazine compound and preparation and medical application thereof
  • Fluorobenzyl substituted piperazine compound and preparation and medical application thereof
  • Fluorobenzyl substituted piperazine compound and preparation and medical application thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0018] Example 1: Preparation of 2-(4-(4-fluorobenzyl)-piperazin-1-yl)-ethylamine

[0019] 1.1 Instruments and reagents

[0020] 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 ...

Embodiment 2

[0026] Example 2: Detection of fungal activity of fluorobenzyl substituted piperazine compounds

[0027] With reference to the standardized antifungal susceptibility test method proposed by the National Committee for Clinical Laboratory Standards (NCCLS), the 2-(4-(4-fluorobenzyl)-piperazin-1-yl)-B In vitro antifungal activity of amines.

[0028] 2.1 Fungal standard strain:

[0029]Candida albicans ATCC10231: Provided by Chongqing Center for Disease Control;

[0030] Candida albicans ATCC90029 (5-FC drug-resistant strain): Provided by the Clinical Laboratory Center of the Ministry of Health of Beijing Hospital;

[0031] Candida albicans 98001: provided by Wuhan Culture Collection Center;

[0032] Candida albicans ATCC76615:19 (Y0119) and ATCC76615:09 (Y0109): Provided by Nanjing Institute of Dermatology.

[0033] 2.2 Reagents:

[0034] 2.2.1 Sabouraud dextrose agar medium (sabouraud dextrose agar): product of Guangdong Kai Microbiology Technology Co., Ltd.

[0035] 2.2...

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Abstract

The invention relates to a fluorobenzyl substituted piperazine compound and preparation and medical application thereof, and specifically discloses 2-(4-(4-fluorobenzyl)-piperazine-1-yl)-ethylamine or a medicinal salt thereof and a preparation method and medical application thereof. The synthesis steps of the compound are simple, the preparation method is simple and easy to implement, the raw materials are convenient and easily available, the cost is low, and little pollution is caused. The fluorobenzyl substituted piperazine compound has obvious inhibitory activity on the growth of fungi, and the MIC value is 62.5-125mg / ml. The result of pharmacodynamics indicates that the fluorobenzyl substituted piperazine compound or the medicinal salt thereof can be expected to serve as a medicine for preventing and treating the diseases caused by fungal infection.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a fluorobenzyl-substituted piperazine compound having antifungal activity, a preparation method thereof, a pharmaceutical composition containing the compound and its use in the preparation of antifungal infection drugs use. 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 seri...

Claims

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Application Information

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IPC IPC(8): C07D295/13A61K31/495A61P31/10
Inventor 白丽吴利先高鹏肖培云张成桂赵昱钱金栿
Owner DALI UNIV
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