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Application of composition of derivatives of Artalbic acid in preparation of antibacterial drugs

A technology of antibacterial drugs and compositions, applied in the fields of organic synthesis and medicinal chemistry, can solve the problems of difficulty in tuberculosis prevention and control, and non-standard treatment and management of tuberculosis patients.

Inactive Publication Date: 2016-10-26
南京海澳斯生物医药科技有限公司
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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 derivatives of Artalbic acid in preparation of antibacterial drugs
  • Application of composition of derivatives of Artalbic acid in preparation of antibacterial drugs
  • Application of composition of derivatives of Artalbic acid in preparation of antibacterial drugs

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Experimental program
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Effect test

Embodiment 1

[0017] The preparation of embodiment 1 compound Artalbic acid

[0018] 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.

[0019]

Embodiment 2

[0020] Synthesis of O-bromoethyl derivative (II) of embodiment 2 Artalbic acid

[0021] 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

[0026] The synthesis of the O-(dichloroethylamino) ethyl derivative (III) of embodiment 3 Artalbic acid

[0027] 1. Synthesis of O-(dihydroxyethylamino)ethyl derivatives of Artalbic acid

[0028] Compound II (187 mg, 0.5 mmol) was dissolved in 20 mL of acetonitrile, anhydrous potassium carbonate (690 mg, 5.0 mmol), potassium iodide (252 mg, 1.5 mmol) and diethanolamine (1051 mg, 10 mmol) were added thereto, and the mixture was heated to reflux for 1 h. After the reaction was completed, 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. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), and the ...

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Abstract

The invention discloses application of a composition of O-(dichloroethylamino)ethyl and O-(di(2-methylthioethyl)amino)ethyl derivatives of Artalbic acid in antibacterial drugs, relates to the field of organic synthesis and medicinal chemistry and particularly relates to a composition of O-(dichloroethylamino)ethyl and O-(di(2-methylthioethyl)amino)ethyl derivatives of Artalbic acid, a preparation method and application thereof in preparation of antibacterial drugs. The invention discloses a composition of O-(dichloroethylamino)ethyl and O-(di(2-methylthioethyl)amino)ethyl derivatives of Artalbic acid and a preparation method thereof. Pharmacological experiments indicate that the composition of O-(dichloroethylamino)ethyl and O-(di(2-methylthioethyl)amino)ethyl derivatives of Artalbic acid has an antibacterial effect and a value of developing 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): A61K31/195A61P31/04A61P31/06A61P31/10A61P1/04
CPCA61K31/195A61K2300/00Y02A50/30
Inventor 丁秋菊
Owner 南京海澳斯生物医药科技有限公司
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