Composition and application thereof to anti-inflammatory drugs

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

Inactive Publication Date: 2016-06-01
CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
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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 co...

Method used

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  • Composition and application thereof to anti-inflammatory drugs
  • Composition and application thereof to anti-inflammatory drugs
  • Composition and application thereof to anti-inflammatory drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] The preparation of embodiment 1 compound Schiglautone A

[0015] The preparation method of the compound Schiglautone A (I) refers to the method published by Fan-Yu Mengetal.

[0016]

Embodiment 2

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

[0018] Compound I (502 mg, 1.00 mmol) was dissolved in 15 mL of benzene, and 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 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=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (508mg, 71%) ...

Embodiment 3

[0023] Synthesis of O-(morpholinyl) ethyl derivative (III) of embodiment 3 Schiglautone A

[0024] Compound II (358 mg, 0.5 mmol) was dissolved in 20 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (168 mg, 1.0 mmol) and morpholine (3484 mg, 40 mmol) were added thereto, and the mixture was heated to reflux for 4 h. After the reaction was completed, the reaction solution was poured into 20 mL of ice water, extracted twice 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), the yellow concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compou...

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Abstract

The invention relates to the field of organic synthesis and medicinal chemistry, in particular to a composition, a preparing method and application thereof to preparation of anti-inflammatory drugs. The invention discloses a composition and a preparing method thereof. The pharmacology experiments show that the composition has an anti-inflammatory function and has value of developing the anti-inflammatory 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] 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): A61K31/5375A61K31/195A61P29/00
CPCA61K9/4866A61K31/195A61K31/5375A61K2300/00
Inventor 华子春吴俊华黄蓉王慧
Owner CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
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