Orixine derivative and application of orixine derivative in preparation of medicine for resisting drug-fast bacteria

A technology of derivatives and persine, which is applied in the field of preparation of anti-drug-resistant bacteria drugs, can solve the problems of antibacterial drugs that have not been reported in the literature, and achieve a strong inhibitory effect

Active Publication Date: 2014-08-13
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the development of antibacterial drugs based on t...

Method used

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  • Orixine derivative and application of orixine derivative in preparation of medicine for resisting drug-fast bacteria
  • Orixine derivative and application of orixine derivative in preparation of medicine for resisting drug-fast bacteria
  • Orixine derivative and application of orixine derivative in preparation of medicine for resisting drug-fast bacteria

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: 3-[3-(3-Hydroxy-2-piperidinyl)-2-oxopropyl]-6-methoxy-7-(1-methylpiperidine-4-methoxy) Synthesis of -4(3H)-quinazolinone

[0033] Towards Potassium tert-butoxide (0.74g, 6.0mmol) was added to anhydrous tetrahydrofuran solution of (1.78g, 5.0mmol), and heated to reflux for 1h. After cooling, a mixture of NBS (1.07 g, 6.0 mmol) in acetonitrile and water (5 ml each) was added, and stirred at room temperature for 0.5 h. Add 100ml of sodium thiosulfate aqueous solution (mass fraction 10%), extract with 100ml of ethyl acetate, wash, dry, filter and concentrate with 6-methoxyl-7-(1-methylpiperidine-4-methyl Oxy)-4(3H)-quinazolinone (1.82g, 6.0mmol) and anhydrous potassium carbonate (0.83g, 6.0mmol) were added to anhydrous DMF (10ml), and stirred at room temperature for 1h. Saturated brine (100 ml) was added, followed by extraction twice with ethyl acetate (50 ml). The organic layer was washed with saturated brine (50ml), dried, filtered, concentrated and purifi...

Embodiment 2

[0036] Example 2: 7-benzyloxy-6-methoxy-3-[3-(3-hydroxyl-2-piperidinyl)-2-oxopropyl]-4(3H)-quinazolinone synthesis

[0037] Towards Potassium tert-butoxide (0.74g, 6.0mmol) was added to anhydrous tetrahydrofuran solution of (1.78g, 5.0mmol), and heated to reflux for 1h. After cooling, a mixture of NBS (1.07 g, 6.0 mmol) in acetonitrile and water (5 ml each) was added, and stirred at room temperature for 0.5 h. Add 100ml of sodium thiosulfate aqueous solution (mass fraction 10%), extract with 100ml of ethyl acetate, wash, dry, filter and concentrate with 7-benzyloxy-6-methoxyl-4(3H)-quinazole Linone (1.70g, 6.0mmol) and anhydrous potassium carbonate (0.83g, 6.0mmol) were added to anhydrous DMF (10ml), and stirred at room temperature for 1h. Saturated brine (100 ml) was added, followed by extraction twice with ethyl acetate (50 ml). The organic layer was washed with saturated brine (50ml), dried, filtered, concentrated and purified by column chromatography. The purified pro...

Embodiment 3

[0040] Example 3: 7-(3-diethylaminopropoxy)-6-methoxy-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]–4(3H )-The synthetic method of quinazolinone

[0041] Towards Potassium tert-butoxide (0.74g, 6.0mmol) was added to anhydrous tetrahydrofuran solution of (1.78g, 5.0mmol), and heated to reflux for 1h. After cooling, a mixture of NBS (1.07 g, 6.0 mmol) in acetonitrile and water (5 ml each) was added, and stirred at room temperature for 0.5 h. Add 100ml of sodium thiosulfate aqueous solution (mass fraction 10%), extract with 100ml of ethyl acetate, wash, dry, filter and concentrate with 7-(3-dimethylaminopropoxy)-6-methoxy- 4(3H)-Quinazolinone (1.83g, 6.0mmol) and anhydrous potassium carbonate (0.83g, 6.0mmol) were added to anhydrous DMF (10ml), and stirred at room temperature for 1h. Saturated brine (100 ml) was added, followed by extraction twice with ethyl acetate (50 ml). The organic layer was washed with saturated brine (50ml), dried, filtered, concentrated and purified by...

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PUM

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Abstract

The invention discloses an orixine derivative and an application of orixine derivative in preparation of medicine for resisting drug-fast bacteria, the test shows that the orixine derivative is capable of inhibiting breeding of a plurality of drug-fast bacterium in vitro, and can be used for preparing antibiotic medicines for resisting drug-fast bacteria; the orixine derivative is used for preparing medicines for resisting methicillin-resistant staphylococcus aureus (MRSA), preparing medicines for resisting benzylpenicillin-resistant staphylococcus aureus, and preparing medicines for resisting vancomycin-resistant enterococcus; the medicines can be prepared to the injection, tablet, pill, capsule, a suspending agent or an emulsion for usage, a chemical structural formula of the orixine derivative is shown in formula I, wherein R1,R2 and R3 are defined in a specification.

Description

technical field [0001] The present invention relates to fusherine derivatives and their application in the preparation of drugs against drug-resistant bacteria. Background technique [0002] Antibacterial drugs are currently the most commonly used class of drugs for the treatment of bacterial infections. Over the years, with the popularization and application of antibiotics around the world, as well as serious irrational abuse, a variety of drug-resistant strains have emerged in both Gram-positive and Gram-negative bacteria. Among them, the problem of drug resistance of Gram-positive bacteria is particularly serious. Methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE) appearing worldwide, Penicillin-resistant Streptococcus pneumoniae (PRSP) and vancomycin-resistant Enterococci (VRE) are serious problems in current clinical practice. Currently, there is a lack of effective treatments for infections caused by these drug-resistant bacteria...

Claims

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Application Information

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IPC IPC(8): C07D401/14C07D401/06C07D417/14C07D513/04A61K31/517A61P31/04
CPCC07D401/06C07D401/14C07D417/14C07D513/04
Inventor 卢宇靖张焜黄宝华杜志云庄子翀雷琳付成杰胡冬萍邓强王郑亚
Owner GUANGDONG UNIV OF TECH
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