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Composition and application thereof in anti-inflammatory drug

A composition and drug technology, applied in the direction of anti-inflammatory agents, drug combinations, active ingredients of heterocyclic compounds, etc., can solve the problems of high toxicity and low safety

Inactive Publication Date: 2016-02-24
NANJING FUHAIAOSAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing drugs for the treatment of inflammation have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs with high efficiency and low toxicity

Method used

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  • Composition and application thereof in anti-inflammatory drug
  • Composition and application thereof in anti-inflammatory drug
  • Composition and application thereof in anti-inflammatory drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] The preparation of embodiment 1 compound SalviskinoneA

[0015] 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, aditerpenewithanewskeleton from Salviaprzewalskii. Tetrahedron Letters 52 (2011) 1375-1377).

[0016]

Embodiment 2

[0017] The synthesis of the O-bromoethyl derivative (II) of embodiment 2SalviskinoneA

[0018] 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

[0023] The synthesis of the O-(piperazinyl) ethyl derivative (III) of embodiment 3SalviskinoneA

[0024] Compound II (209mg, 0.5mmol) was dissolved in 25mL of acetonitrile, anhydrous potassium carbonate (690mg, 5.0mmol), potassium iodide (168mg, 1.0mmol) and anhydrous piperazine (3446mg, 40mmol) were added thereto, and the mixture was heated to reflux 6h. After the reaction, 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), the brown concentrated elution band was collected and the solvent was evaporated to obtain compound III as a light brown solid (15...

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Abstract

The invention relates to the fields of organic synthesis and medicinal chemistry, and in particular relates to a composition, a preparation method and application of the composition in preparing an anti-inflammatory drug. The invention discloses a composition and a preparation method thereof. Based upon pharmacological experiments, the composition disclosed by the invention has an anti-inflammatory effect, so that the composition has the value of developing the anti-inflammatory drug.

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] Inflammation occurs locally but can also affect the whole body. Local clinical features are redness, heat, swelling, pain and dysfunction. Redness and heat are due to the expansion of local blood vessels and the acceleration of blood flow due to inflammation. Swelling is caused by local inflammatory hyperemia and exudation of blood flow components. The development of drugs with anti-inflammatory effects is of great significance for the verification of relief and pain relief. [0003] The existing drugs for the treatment of inflammation have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/495A61K31/41A61P29/00C07D295/088C07D257/04
CPCA61K31/41A61K31/495C07D257/04C07D295/088A61K2300/00
Inventor 王卓婷
Owner NANJING FUHAIAOSAI PHARMA CO LTD
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