Application of composition of derivative of Schiglautone A in antibacterial agents

A technology of antibacterial drugs and compositions, applied in the fields of organic synthesis and medicinal chemistry, can solve problems such as difficulties in tuberculosis prevention and control, and non-standard treatment and management of tuberculosis patients

Inactive Publication Date: 2017-02-22
NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the irregular treatment and management of tuberculosis patients, irregular chemotherapy and abuse of anti-tuberculosis drugs, the drug resistance

Method used

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  • Application of composition of derivative of Schiglautone A in antibacterial agents
  • Application of composition of derivative of Schiglautone A in antibacterial agents
  • Application of composition of derivative of Schiglautone A in antibacterial agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The preparation of embodiment 1 compound Schiglautone A

[0019] The preparation method of compound Schiglautone A (I) refers to the literature published by Fan-Yu Meng et al. of Schisandra glaucescens. Organic Letters 13 (2011) 1502–1505).

[0020]

Embodiment 2

[0021] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Schiglautone A

[0022] Compound I (502 mg, 1.00 mmol) was dissolved in 15 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 8 h. After 8 hours, the reaction solution was poured into ice water, extracted twice with dichloromethane immediately, and the organic phase solutions were combined. Then the organic phase solution was washed with water and saturated brine three times successively, then dried with anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (508mg, 71%...

Embodiment 3

[0027] The synthesis of the O-(triazolyl) ethyl derivative (III) of embodiment 3 Schiglautone A

[0028] Compound II (358mg, 0.5mmol) was dissolved in 10mL of acetonitrile, anhydrous potassium carbonate (345mg, 2.5mmol), potassium iodide (84mg, 0.5mmol) and 1,2,3-triazole (2760mg, 40mmol) were added ), the mixture was heated to reflux for 3h. After the reaction, the reaction solution was poured into ice water, extracted twice with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were successively washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), and the light yellow concentrated elution band was collected to obtain compound III as a yellow colloidal solid (245.7mg, 71%) .

[0029] 1H NMR(5...

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PUM

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Abstract

The invention relates to the field of organic synthesis and pharmaceutical chemistry, in particular to compositions, preparing methods and applications of the compositions in preparing antibacterial agents. The invention discloses a composition and a preparing method thereof. Pharmacology experiments indicate that the composition has an antibacterial effect and has a value in the development of antibacterial agents.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method and an application thereof. Background technique [0002] The spread of pathogenic bacteria and the enhancement of drug resistance seriously threaten human health and life. Antibacterial drugs have been widely used as routine drugs in the treatment of AIDS, organ transplantation and chronic wasting diseases (such as cancer, diabetes, uremia, etc.) Treatment, although antibacterial agents currently used clinically (such as ketoconazole, amikacin, gentamicin, vigorconazole, itraconazole, terbinafine, amphotericin, fluconazole, etc.) The curative effect on skin and superficial infection is good, but these antibacterial drugs have strong accumulation toxicity, often causing liver and kidney damage, gastrointestinal irritation, dizziness, allergies, etc. one of the hotspots. [0003] Helicobacter pylori (Hp) is a Gram-nega...

Claims

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Application Information

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IPC IPC(8): A61K31/4192A61K31/195C07D249/04C07C323/25A61P31/04A61P31/06
CPCA61K31/195A61K31/4192C07C323/25C07D249/04A61K2300/00Y02A50/30
Inventor 陆贤
Owner NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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