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Ergosta-7,22-dien-3-ketothiazide and its preparation method and application in the preparation of antibacterial drugs

A technology of ketal thizone and ergoster, which is applied in the directions of antibacterial drugs, steroids, organic chemistry, etc., can solve the problems that have not been seen before, and achieves the effects of abundant sources and simple preparation process

Inactive Publication Date: 2020-02-14
FOSHAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But so far, there is no report about ergosta-7,22-dien-3-ketone thizone and its preparation method and application in the preparation of antibacterial drugs

Method used

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  • Ergosta-7,22-dien-3-ketothiazide and its preparation method and application in the preparation of antibacterial drugs
  • Ergosta-7,22-dien-3-ketothiazide and its preparation method and application in the preparation of antibacterial drugs
  • Ergosta-7,22-dien-3-ketothiazide and its preparation method and application in the preparation of antibacterial drugs

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] 1. Preparation of Compound A:

[0037] (1) Take 0.50mmol ergosta-7,22-dien-3-one, dissolve it with 10mL petroleum ether and set aside;

[0038] (2) Add 0.60mmol thiosemicarbazide and 50mL absolute ethanol in the two-necked round-bottomed flask, insert a magnetic stirrer, install a spherical condenser, plug the other mouth with a hollow glass stopper, connect cooling water, and Heating to slight boiling under magnetic stirring to completely dissolve thiosemicarbazide, then add the petroleum ether solution of ergosta-7,22-dien-3-one, and add 5 drops of concentrated hydrochloric acid, continue to stir and heat to reflux for 4 hours, use silica gel TLC tracking until the reaction is complete;

[0039] (3) After the reaction is completed, most of the solvent is recovered by vacuum rotary evaporation at 50° C., then 50 mL of distilled water is added, and extracted three times with an equal volume of ethyl acetate;

[0040] (4) The ethyl acetate extracts were combined, washe...

Embodiment 2

[0047] Compound A was prepared according to Example 1, and excipients were added according to the mass ratio of compound crystals and excipients at a ratio of 1:1, and then granulated and compressed into tablets.

Embodiment 3

[0049] Compound A was prepared according to Example 1, and excipients were added according to the mass ratio of compound crystals and excipients at a ratio of 1:2, and then granulated and compressed into tablets.

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Abstract

The invention discloses ergosterol-7,22-diene-3-keto-thiosemicarbazone hydrazone, a preparation method of same, and an application thereof in preparation of antibacterial medicines. The ergosterol-7,22-diene-3-keto-aminothiohydrazone is a novel ergosterol-type natural product derivative and can be prepared through a condensation reaction to ergosterol-7,22-diene-3-ketone and thiosemicarbazide. Anin-vitro antibacterial test result proves that the ergosterol-7,22-diene-3-keto-thiosemicarbazone hydrazone has excellent anti-pathogenic bacteria activity and can be used for preparing antibacterialmedicines.

Description

technical field [0001] The present invention relates to an antibacterial compound, more specifically, the present invention relates to ergosta-7,22-dien-3-one thizone, its preparation method and its application in the preparation of antibacterial drugs. Background technique [0002] In recent years, due to the abuse of antibiotics, many pathogenic bacteria have developed drug resistance and super bacteria have appeared. At the same time, new pathogenic bacteria have emerged continuously, which seriously threaten human health. There is an urgent need to develop new antibacterial drugs. Structural modification of natural product leads is one of the important methods for screening new drugs. Steroids widely exist in animals, plants and microorganisms, and have various biological activities. The structural modification of steroids has led to the discovery of many steroid derivatives with good antibacterial and antitumor activities. Ergosta-7,22-dien-3-one widely exists in fru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J41/00A61P31/04
CPCC07J41/0005
Inventor 朱峰唐椅璐梁凯恩吴金玲陈杰华
Owner FOSHAN UNIVERSITY
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