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Application of O-(diethylamino) ethyl derivative of Daphmalenine A in preparation of antibacterial drug

A technology of antibacterial drugs and derivatives, applied in antibacterial drugs, antifungal agents, drug combinations, etc., can solve the problems of non-standard treatment and management of tuberculosis patients, difficulties in tuberculosis prevention and control, and achieve good antibacterial effect.

Inactive Publication Date: 2015-09-02
NANJING UNIV
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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 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 O-(diethylamino) ethyl derivative of Daphmalenine A in preparation of antibacterial drug
  • Application of O-(diethylamino) ethyl derivative of Daphmalenine A in preparation of antibacterial drug
  • Application of O-(diethylamino) ethyl derivative of Daphmalenine A in preparation of antibacterial drug

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The preparation of embodiment 1 compound Daphmalenine A

[0024] The preparation method of compound Daphmalenine A (I) refers to the literature published by Yu Zhang et al. , 4103–4107) approach.

[0025]

Embodiment 2

[0026] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Daphmalenine A

[0027] Compound I (419 mg, 1.00 mmol) was dissolved in 10 mL of benzene, 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 12 h. After 12 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 four 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=100:1.5, v / v), and the yellow concentrated elution band was collected to obtain compound II as a yellow solid (320 mg, 61%).

[0028] 1H NMR (500MHz,...

Embodiment 3

[0032] The synthesis of the O-(diethylamino) ethyl derivative (III) of embodiment 3 Daphmalenine A

[0033] Compound II (263 mg, 0.5 mmol) was dissolved in 20 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (84 mg, 0.5 mmol) and diethylamine (1460 mg, 20 mmol) were added thereto, and the mixture was heated to reflux for 10 h . After the reaction, the reaction solution was poured into ice water, extracted four 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, v / v), and the yellow concentrated elution band was collected to obtain the O-(diethylamino)ethyl derivative of Daphmalenine A (I...

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Abstract

The invention relates to the field of organic synthesis and medicinal chemistry, in particular to a Daphmalenine A derivative, a preparation method and application of the Daphmalenine A derivative in preparation of antibacterial drug. A new Daphmalenine A derivative is synthesized. Pharmacological experiments show that the Daphmalenine A derivative has antibacterial effect and has value in developing the antibacterial drug.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a Daphmalenine A derivative, 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) ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439A61P31/04A61P31/10A61P31/06A61P1/04C07D491/107
CPCY02A50/30
Inventor 吴俊华皋林吴俊艺
Owner NANJING UNIV
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