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Phenytoin derivative as well as preparation method and application thereof

A technology of phenytoin and derivatives, applied in the field of phenytoin derivatives and their preparation, can solve the problems of susceptibility to infection, long wound healing time, affecting the work and life of patients, etc., and achieve good bacteriostatic and bactericidal effects, and the effects of inhibiting wound infection.

Active Publication Date: 2014-09-03
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Most of the traditional wound treatment drugs used clinically are used to inhibit wound infection, and the effect on promoting wound healing is not obvious
Especially for large wounds, the wound takes a long time to heal and is prone to infection, seriously affecting the work and life of patients

Method used

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  • Phenytoin derivative as well as preparation method and application thereof
  • Phenytoin derivative as well as preparation method and application thereof
  • Phenytoin derivative as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment approach

[0017] The invention prepares the compound phenytoin silver through chemical reaction, and identifies the prepared phenytoin silver through infrared absorption spectrum and atomic absorption spectrum. Through a series of experiments, the antibacterial activity and wound healing activity of silver phenytoin were detected. The specific implementation is as follows:

[0018] In the following examples, used test materials and sources thereof include:

[0019] Sodium phenytoin and silver nitrate were purchased from Shanghai Sangon Biological Company, ammonia water was purchased from Tianjin North Tianyi Chemical Reagent Factory, and Escherichia coli was purchased from Tianjin International Pharmaceutical Joint Research High-throughput Drug Screening Center. The beef extract and peptone used in LB medium were purchased from OXOID Company. C57 / BL mice used in the experiment were purchased from the Experimental Animal Center of the Academy of Military Medical Sciences.

Embodiment 1

[0020] Embodiment 1: Synthesis and identification of silver phenytoin

[0021] 1.1 Synthesis of silver phenytoin (see figure 1 )

[0022] Preparation of phenytoin: Dissolve 10 g of phenytoin sodium in water, adjust the pH value to 6 with 10% hydrochloric acid, precipitate a white precipitate, filter with suction, wash the crystals with a small amount of water, and dry in vacuum to obtain dry phenytoin.

[0023] Configuration of silver ammonia solution: weigh 1.68g AgNO 3 Add 2% dilute ammonia water drop by drop to the medium and shake continuously until the initial precipitate just dissolves.

[0024] Synthesis of silver phenytoin: Weigh 2.75 g of dry phenytoin and dissolve it in 50 mL of 2% dilute ammonia water to prepare a phenytoin solution. Under ultrasonic conditions, the above-prepared silver-ammonia solution was added dropwise to 2% ammonia solution of phenytoin, and a white precipitate was formed. The resulting precipitate is silver phenytoin. The precipitate was ...

Embodiment 2

[0029] Embodiment 2 phenytoin silver antibacterial activity test

[0030] 2.1 Experimental method:

[0031] 1) Take 5 μL of Escherichia coli glycerol, inoculate into 5 mL of liquid LB medium, place in a shaker at 37°C, 220 rpm / min, and culture overnight;

[0032] 2) Take 200 μL of Escherichia coli cultured overnight, dilute it 10 times, take 200 μL, and smear it on solid LB medium without antibody;

[0033] 3) Cut the filter paper into discs with a diameter of 1 cm, immerse in distilled water and sterilize by autoclaving;

[0034] 4) Divide the culture medium full of Escherichia coli into four parts, two parts are the experimental group, and two parts are the control group. In the experimental group, a filter paper dipped in silver phenytoin suspension was pasted on the bacteria, and in the control group, a filter paper dipped in sterile distilled water was pasted. After 24 hours, observe whether there is an antibacterial zone formed around the filter paper of the experimen...

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Abstract

The invention provides a phenytoin derivative with a structure (I), a preparation method of the phenytoin derivative, application of the phenytoin derivative to preparation of externally-applied medicaments for promoting wound healing and inhibiting bacterial wound infection, and the externally-applied medicaments for promoting the wound healing and inhibiting the wound infection. The structure (I) is as shown the specification.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to phenytoin derivatives and their preparation methods and applications. Background technique [0002] The skin is the largest organ of the human body. It protects various tissues and organs in the body from physical, mechanical, chemical and pathogenic microorganisms. When the skin is damaged and the wound is large, it is difficult to heal quickly, which will lead to the invasion of external viruses and harmful substances into the human body, causing symptoms such as infection and suppuration of the wound. Factors such as skin infection can make wound healing difficult. At the same time, wound infection will cause the defense mechanism in the human body to respond, triggering a series of inflammatory and other reactions. [0003] Most of the traditional wound treatment drugs used clinically are used to inhibit wound infection, and the effect on promoting wound heali...

Claims

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Application Information

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IPC IPC(8): C07D233/74A61K31/4166A61P17/02A61P31/04
CPCC07D233/74Y02A50/30
Inventor 孙涛杨诚周红刚尹正
Owner NANKAI UNIV
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