Application of composition of O-(lignocaine) ethyl derivative and O-(piperazinyl) ethyl derivative of Harrisotone A in antibacterial agents

An antibacterial drug and composition technology, which can be applied in the directions of antibacterial drugs, antifungal agents, and medical preparations containing active ingredients, etc., can solve problems such as difficulties in tuberculosis prevention and control, and the treatment and management of tuberculosis patients are not very standardized.

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 of tuberculosis is becoming more and more serious, and the change of drug resistance tends to be multi-drug resistance at the same time. great difficulty at work

Method used

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  • Application of composition of O-(lignocaine) ethyl derivative and O-(piperazinyl) ethyl derivative of Harrisotone A in antibacterial agents
  • Application of composition of O-(lignocaine) ethyl derivative and O-(piperazinyl) ethyl derivative of Harrisotone A in antibacterial agents
  • Application of composition of O-(lignocaine) ethyl derivative and O-(piperazinyl) ethyl derivative of Harrisotone A in antibacterial agents

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The preparation of embodiment 1 compound Harrisotone A

[0019] The preparation method of compound Harrisotone A (I) refers to the literature published by Sheng Yin et al. (Sheng Yin et al., 2009.Harrisotones A–E, five novel prenylated polyketides with a rarespirocyclic skeleton from Harrisonia perforata.Tetrahedron 65(2009) 1147–1152 )Methods.

[0020]

Embodiment 2

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

[0022] Compound I (472 mg, 1.00 mmol) was dissolved in 15 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (3.760 g, 20.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 3 h. After 3h, 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 twice with water and saturated brine 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=100:1.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a yellow powder of compound II (602mg, 76%) .

[00...

Embodiment 3

[0026] The synthesis of the O-(diethylamino) ethyl derivative (III) of embodiment 3 Harrisotone A

[0027] Compound II (396mg, 0.5mmol) was dissolved in 15mL of acetonitrile, anhydrous potassium carbonate (345mg, 2.5mmol), potassium iodide (84mg, 0.5mmol) and diethylamine (2920mg, 40mmol) were added thereto, and 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=100:1.5, v / v), and the concentrated brown elution band was collected and concentrated to give Compound III as a pale yellow solid (246.1mg, 64%) .

[0...

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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): A61K31/495A61K31/132A61P31/04A61P31/06A61P31/10
CPCA61K31/132A61K31/495A61K2300/00Y02A50/30
Inventor 陆贤
Owner NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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