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Application of composition of Salviskinone A benzimidazolyl and di(2-methylmercapto ethyl)amido derivatives in antibacterial drugs

A technology of antibacterial drugs and compositions, applied in the direction of antibacterial drugs, drug combinations, 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: 2016-10-12
NANJING FUHAIAOSAI PHARMA CO LTD
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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 Salviskinone A benzimidazolyl and di(2-methylmercapto ethyl)amido derivatives in antibacterial drugs
  • Application of composition of Salviskinone A benzimidazolyl and di(2-methylmercapto ethyl)amido derivatives in antibacterial drugs
  • Application of composition of Salviskinone A benzimidazolyl and di(2-methylmercapto ethyl)amido derivatives in antibacterial drugs

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The preparation of embodiment 1 compound Salviskinone A

[0019] The preparation method of the compound Salviskinone A (I) refers to the method published by Ayumi Ohsaki et al. (Ayumi Ohsaki et al., 2011. Salviskinone A, a diterpene with a new skeleton from Salviaprzewalskii. Tetrahedron Letters 52 (2011) 1375-1377).

[0020]

Embodiment 2

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

[0022] Compound I (312 mg, 1.00 mmol) was dissolved in 15 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 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), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (327mg, 78...

Embodiment 3

[0027] Example 3 Synthesis of O-(benzimidazolyl)ethyl derivative (III) of Salviskinone A

[0028] Compound II (209mg, 0.5mmol) was dissolved in 20mL of acetonitrile, anhydrous potassium carbonate (345mg, 2.5mmol), potassium iodide (84mg, 0.5mmol) and benzimidazole (1180mg, 10mmol) were added thereto, and the mixture was heated to reflux for 5h . 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=100:1.5, v / v), and the concentrated brown elution band was collected and concentrated to give compound III as a brown solid (215 mg, 43%).

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Abstract

The invention discloses an application of a composition of Salviskinone A benzimidazolyl and di(2-methylmercapto ethyl)amido derivatives in antibacterial drugs, relates to the fields of organic synthesis and medicinal chemistry, and particularly relates to the composition of the Salviskinone A benzimidazolyl and di(2-methylmercapto ethyl)amido derivatives, and a preparation method and the application thereof in preparation of the antibacterial drugs. Provided are the composition of the Salviskinone A benzimidazolyl and di(2-methylmercapto ethyl)amido derivatives and the preparation method thereof. Pharmacological experiments indicate that the composition has an antibacterial effect and has the value for development of the 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): A61K31/4184A61K31/145C07D235/08C07C323/25A61P31/04A61P31/06A61P31/10A61P1/04
CPCA61K31/145A61K31/4184C07C323/25C07D235/08A61K2300/00Y02A50/30
Inventor 王卓婷
Owner NANJING FUHAIAOSAI PHARMA CO LTD
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