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Use of composition of triazolyl derivative and 1H-tetrazolyl derivative of Artalbic acid in preparation of antibacterial medicines

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: 2016-11-09
南京海澳斯生物医药科技有限公司
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  • 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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  • Use of composition of triazolyl derivative and 1H-tetrazolyl derivative of Artalbic acid in preparation of antibacterial medicines
  • Use of composition of triazolyl derivative and 1H-tetrazolyl derivative of Artalbic acid in preparation of antibacterial medicines
  • Use of composition of triazolyl derivative and 1H-tetrazolyl derivative of Artalbic acid in preparation of antibacterial medicines

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Effect test

Embodiment 1

[0018] The preparation of embodiment 1 compound Artalbic acid

[0019] The preparation method of compound Artalbic acid (I) refers to the literature published by Antonella Maggio et al. (Antonella Maggio et al., 2011. Artalbic acid, a sesquiterpene with an unusual skeleton from Artemisia alba (Asteraceae) from Sicily. Tetrahedron Letters, 52 (2011) 4543–4545) approach.

[0020]

Embodiment 2

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

[0022] Compound I (266 mg, 1.00 mmol) was dissolved in 10 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 40 °C for 16 h. After 16 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 for 5 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 (272mg, 73...

Embodiment 3

[0027] Synthesis of O-(triazolyl) ethyl derivative (III) of embodiment 3 Artalbic acid

[0028] Compound II (187mg, 0.5mmol) was dissolved in 25mL 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 was completed, the reaction solution was poured into 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. 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 light yellow colloidal solid (124.5mg, 69% ).

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Abstract

The invention relates to an application of a composition of the O-(triazolyl)ethyl derivative and the O-(1H-tetrazolyl)ethyl derivative of Artalbic acid in the preparation of antibacterial medicines, relates to the fields of organic synthesis and pharmaceutical chemistry, and concretely relates to the composition of the O-(triazolyl)ethyl derivative and the O-(1H-tetrazolyl)ethyl derivative of Artalbic acid, and a use of the composition in the preparation of the antibacterial medicines. The invention discloses the composition of the O-(triazolyl)ethyl derivative and the O-(1H-tetrazolyl)ethyl derivative of Artalbic acid, and the preparation method thereof. Pharmacologic experiments show that the composition of the O-(triazolyl)ethyl derivative and the O-(1H-tetrazolyl)ethyl derivative of Artalbic acid has an antibacterial effect, and has values in exploitation of the antibacterial medicines.

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): A61K31/4192A61K31/41A61P31/04A61P31/06A61P31/10
CPCA61K31/41A61K31/4192A61K2300/00Y02A50/30
Inventor 丁秋菊
Owner 南京海澳斯生物医药科技有限公司
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