Composition 77083001030592 and application thereof in antibacterial drugs

An antibacterial drug and composition technology, which can be used in antibacterial drugs, antifungal agents, and resistance to vector-borne diseases, etc., can solve the problems of non-standard treatment and management of tuberculosis patients and difficulties in tuberculosis prevention and control work.

Inactive Publication Date: 2015-11-25
苏州贺澳德生物医药科技有限公司
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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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  • Composition 77083001030592 and application thereof in antibacterial drugs
  • Composition 77083001030592 and application thereof in antibacterial drugs
  • Composition 77083001030592 and application thereof in antibacterial drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The preparation of embodiment 1 compound PsiguadialA

[0019] The preparation method of the compound PsiguadialA (I) refers to the method published by Meng Shao et al. (Meng Shao et al., 2010. Psiguadials A and B, Two Novel Meroterpenoids with Unusual Skeletons from the Leaves of Psidiumguajava. Organic Letters 12 (2010) 5040-5043).

[0020]

Embodiment 2

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

[0022] Compound I (474 ​​mg, 1.00 mmol) was dissolved in 20 mL of benzene, tetrabutylammonium bromide (TBAB) (0.16 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 12 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=100:0.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (502mg, 73%) . ...

Embodiment 3

[0027] The synthesis of the O-(diethylamino) ethyl derivative (III) of embodiment 3PsiguadialA

[0028] Compound II (344mg, 0.5mmol) was dissolved in 20mL of acetonitrile, anhydrous potassium carbonate (690mg, 5.0mmol), potassium iodide (168mg, 1.0mmol) and diethylamine (2920mg, 40mmol) were added thereto, and the mixture was heated to reflux for 9h . After the reaction, the reaction solution was poured into ice water, extracted 4 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=100:1.5, v / v), the yellow concentrated elution band was collected and the solvent was evaporated to obtain a yellow powder of compound III (231.8mg, 69% ...

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Abstract

The present invention relates to the fields of organic synthesis and medicine chemistry, and in particular relates to a composition 77083001030592, a preparation method and application thereof in preparing antibacterial drugs. The present invention discloses a composition 77083001030592 and a preparation method thereof. Pharmacological experiments show that the composition 77083001030592 has antibacterial effect, and the value in development of antibiotics.

Description

technical field [0001] The present invention relates to the fields of organic synthesis and medicinal chemistry, in particular to composition 77083001030592, a preparation method and its application. 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): A61K31/4545A61P31/04A61P31/10A61P31/06A61K31/335
CPCY02A50/30
Inventor 朱磊磊
Owner 苏州贺澳德生物医药科技有限公司
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