Application of composition of Schiglautone A derivatives in preparation of antibacterial drugs

A technology of antibacterial drugs and compositions, applied in the direction of antibacterial drugs, medical preparations containing active ingredients, antifungal agents, etc., which can solve the problems of non-standard treatment and management of tuberculosis patients and difficulties in tuberculosis prevention and control work

Inactive Publication Date: 2016-10-26
NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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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 resistan...

Method used

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  • Application of composition of Schiglautone A derivatives in preparation of antibacterial drugs
  • Application of composition of Schiglautone A derivatives in preparation of antibacterial drugs
  • Application of composition of Schiglautone A derivatives in preparation of antibacterial drugs

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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] Synthesis of O-(1H-tetrazolyl)ethyl derivative (III) of Schiglautone A of embodiment 3

[0028] Compound II (358 mg, 0.5 mmol) was dissolved in 15 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (84 mg, 0.5 mmol) and 1H-tetrazolium (1401 mg, 20 mmol) were added thereto, and the mixture was heated Reflux for 5h. After the reaction, the reaction solution was poured into 20 mL of ice water, extracted three times 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. Because of tautomerism, two substitution products, 1H-tetrazolyl and 2H-tetrazolyl, will be generated under the reaction conditions. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=1...

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Abstract

The invention relates to the field of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method of the composition and application of the composition in the preparation of antibacterial drugs. The invention also discloses a composition and a preparation method thereof. Pharmacological experiments show that the composition of the invention is antibacterial and is worthy of being developed into 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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IPC IPC(8): A61K31/4184A61K31/41A61P31/10A61P31/04A61P31/06C07D257/04C07D235/06
CPCA61K31/41A61K31/4184C07D235/06C07D257/04A61K2300/00Y02A50/30
Inventor 陆贤
Owner NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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