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Composition and application thereof to antibacterial medicines

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

Inactive Publication Date: 2016-02-03
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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  • Composition and application thereof to antibacterial medicines
  • Composition and application thereof to antibacterial medicines
  • Composition and application thereof to antibacterial medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] The preparation of embodiment 1 compound Artalbicacid

[0018] The preparation method of compound Artalbicacid (I) refers to the method published by Antonella Maggio et al. (Antonella Maggio et al., 2011. Artalbicacid, asesquiterpenewithanunusualskeletonfromArtemisiaalba (Asteraceae) fromSicily.TetrahedronLetters, 52 (2011) 4543-4545).

[0019]

Embodiment 2

[0020] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Artalbicacid

[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] Synthesis of O-(piperazinyl) ethyl derivative (III) of embodiment 3 Artalbicacid

[0027] Compound II (187mg, 0.5mmol) was dissolved in 25mL of acetonitrile, anhydrous potassium carbonate (345mg, 2.5mmol), potassium iodide (84mg, 0.5mmol) and anhydrous piperazine (3446mg, 40mmol) were added thereto, and the mixture was heated to reflux 4h. 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=100:1.5, v / v), the light brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compoun...

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Abstract

The invention relates to the field of organic synthesis and medicinal chemistry and in particular relates to a composition, a preparation method and an application of the composition to preparation of antibacterial medicines. The invention discloses the composition and the preparation method thereof. Pharmacological experiments show that the composition has the antibacterial effect and has the value in developing 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): A61K31/495A61P31/04A61P31/10A61P31/06A61K31/4164
CPCY02A50/30
Inventor 丁秋菊
Owner 南京海澳斯生物医药科技有限公司
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