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Composition and application thereof to antibacterial drugs

A technology of antibacterial drugs and compositions, which can be applied in the direction of antibacterial drugs, antifungal agents, and resistance to vector-borne diseases, etc., and can solve problems such as difficulties in tuberculosis prevention and control, and non-standard treatment and management of tuberculosis patients.

Inactive Publication Date: 2016-01-13
CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • Composition and application thereof to antibacterial drugs
  • Composition and application thereof to antibacterial drugs
  • Composition and application thereof to antibacterial drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The preparation of embodiment 1 compound Schiglautone A

[0019] The preparation method of the compound Schiglautone A (I) refers to the method published by Fan-Yu Mengetal.

[0020]

Embodiment 2

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

[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-(diethylamino) ethyl derivative (III) of embodiment 3 Schiglautone A

[0028] Compound II (358mg, 0.5mmol) was dissolved in 10mL of acetonitrile, anhydrous potassium carbonate (690mg, 5.0mmol), potassium iodide (168mg, 1.0mmol) and diethylamine (2920mg, 40mmol) were added thereto, and the mixture was heated to reflux for 8h . 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), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compound III (231.2mg, 66% ...

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Abstract

The invention relates to the fields of organic synthesis and pharmaceutical chemistry, in particular to a composition, a preparing method and application thereof to preparation of antibacterial drugs. The invention discloses the composition and the preparing method thereof. Pharmacology experiments show that the composition has an antibacterial effect and has the value of developing the antibacterial drugs.

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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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/195A61P31/04A61P31/10A61P31/06
CPCY02A50/30
Inventor 华子春吴俊华黄蓉王慧
Owner CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
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