Application of derivative composition of Harrisotone A to anti-inflammation

A composition and compound technology, which can be used in drug combinations, anti-inflammatory agents, medical preparations containing active ingredients, etc., and can solve the problems of high toxicity and low safety.

Inactive Publication Date: 2017-06-13
NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • Application of derivative composition of Harrisotone A to anti-inflammation
  • Application of derivative composition of Harrisotone A to anti-inflammation
  • Application of derivative composition of Harrisotone A to anti-inflammation

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] The preparation of embodiment 1 compound Harrisotone A

[0015] The preparation method of compound Harrisotone A (I) refers to the literature published by Sheng Yin et al. (Sheng Yin et al., 2009.Harrisotones A–E, five novel prenylated polyketides with a rarespirocyclic skeleton from Harrisonia perforata.Tetrahedron 65(2009) 1147–1152 )Methods.

[0016]

Embodiment 2

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

[0018] Compound I (472 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 3 h. After 3h, 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 twice with water and saturated brine 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 yellow powder of compound II (602mg, 76%) .

[00...

Embodiment 3

[0023] The synthesis of the O-(dichloroethylamino) ethyl derivative (III) of embodiment 3 Harrisotone A

[0024] 1. Synthesis of O-(dihydroxyethylamino)ethyl derivatives of Harrisotone A

[0025] Compound II (396 mg, 0.5 mmol) was dissolved in 22 mL of acetonitrile, anhydrous potassium carbonate (690 mg, 5.0 mmol), potassium iodide (252 mg, 1.5 mmol) and diethanolamine (1051 mg, 10 mmol) were added thereto, and the mixture was heated to reflux for 3 h. After the reaction, the reaction solution was poured into 25 mL of 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=100:0.5, v / v), and the light brown co...

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PUM

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Abstract

The invention discloses application of a derivative composition of Harrisotone A to anti-inflammation, namely, application of a composition of an O-(diethylamine chloride)ethyl derivative and an O-di(2-methylmercapto-ethyl)amino derivative of the Harrisotone A to an anti-inflammation medicament. The invention relates to the fields of organic synthesis and pharmaceutical chemistry, in particular to a composition of Harrisotone A derivatives, a preparation method of the composition and application of the composition to preparation of an anti-inflammation medicament. The invention discloses a composition of Harrisotone A derivatives and a preparation method thereof. As proved by a pharmacology experiment, the composition of the Harrisotone A derivatives has an anti-inflammation effect, and has a value of developing the anti-inflammation medicament.

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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IPC IPC(8): A61K31/145A61K31/132A61P29/00C07C217/12C07C323/25
CPCA61K31/145A61K31/132C07C217/12C07C323/25A61K2300/00
Inventor 陆贤江春平
Owner NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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