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Composition and application of composition to antibacterial medicine

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: 2016-06-01
NANJING UNIV
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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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  • Composition and application of composition to antibacterial medicine
  • Composition and application of composition to antibacterial medicine
  • Composition and application of composition to antibacterial medicine

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] Synthesis of O-(morpholinyl) ethyl derivative (III) of embodiment 3 Schiglautone A

[0028] Compound II (358 mg, 0.5 mmol) was dissolved in 20 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (168 mg, 1.0 mmol) and morpholine (3484 mg, 40 mmol) were added thereto, and the mixture was heated to reflux for 4 h. After the reaction was completed, the reaction solution was poured into 20 mL of 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=100:0.5, v / v), the yellow concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compou...

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Abstract

The invention relates to the field of organic synthesis and medicine chemistry, in particular to a composition, a preparation method and application of the composition to preparation of antibacterial medicine. The invention discloses the composition and the preparation method of the composition. Pharmacological experiments show that the composition has the antibacterial effect, and has antibacterial medicine development values.

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): A61K31/5377A61K31/19A61P31/04A61P31/06A61P31/10C07D295/088C07C217/12
CPCA61K31/19A61K31/5377C07C217/12C07D295/088A61K2300/00Y02A50/30
Inventor 吴俊华周未末
Owner NANJING UNIV
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