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Composition and application thereof in drug for preventing or treating pancreatic fibrosis

A technology of pancreatic fibrosis and composition, which is applied in the fields of organic synthesis and medicinal chemistry, and can solve the problems of low safety and high toxicity

Inactive Publication Date: 2016-02-24
南京海澳斯生物医药科技有限公司
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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 pancreatic fibrosis have the problems of high toxicity and low safety. It is most important 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 drug for preventing or treating pancreatic fibrosis
  • Composition and application thereof in drug for preventing or treating pancreatic fibrosis
  • Composition and application thereof in drug for preventing or treating pancreatic fibrosis

Examples

Experimental program
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Effect test

Embodiment 1

[0010] The preparation of embodiment 1 compound Artalbicacid

[0011] The preparation method of compound Artalbicacid (I) refers to the method published by Antonella Maggio et al. (Antonella Maggio et al., 2011. Artalbicacid, asesquiterpenewithanunusualskeletonfromArtemisiaalba (Asteraceae) fromSicily.TetrahedronLetters, 52 (2011) 4543-4545).

[0012]

Embodiment 2

[0013] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Artalbicacid

[0014] Compound I (266 mg, 1.00 mmol) was dissolved in 10 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 40 °C for 16 h. After 16 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 for 5 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 (272mg, 73%...

Embodiment 3

[0019] The synthesis of O-(piperidinyl) ethyl derivative (III) of embodiment 3 Artalbicacid

[0020] Compound II (187 mg, 0.5 mmol) was dissolved in 20 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (84 mg, 0.5 mmol) and piperidine (852 mg, 10 mmol) were added thereto, and the mixture was heated to reflux for 10 h. After the reaction, the reaction solution was poured into 20 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), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compound III (...

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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 a drug for preventing or treating pancreatic fibrosis. The invention discloses a composition and a preparation method thereof. Based upon pharmacological experiments, the composition disclosed by the invention has an effect on preventing or treating the pancreatic fibrosis, so that the composition has the value of developing the drug for preventing or treating the pancreatic fibrosis.

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] Pancreatic fibrosis is a common feature of chronic pancreatitis caused by various reasons, and it is also the accompanying histopathological feature, manifested as a large number of fibroblast proliferation and extracellular matrix rich in connective tissue. It is the result of pancreatic damage and repair due to various reasons. Recently, pancreatic stellate cells and various cytokines have been found to be related to pancreatic fibrosis. The incidence of pancreatic fibrosis is increasing. There is an urgent need to develop effective and low-toxic anti-pancreatic fibrosis drugs. . [0003] The existing drugs for the treatment of pancreatic fibrosis have the problems of high toxicity and low safety. It is most important to find compounds or lead compounds from n...

Claims

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Application Information

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IPC IPC(8): A61K31/5375A61P1/18C07D295/088A61K31/4453
CPCA61K9/4866A61K31/4453A61K31/5375C07D295/088A61K2300/00
Inventor 丁秋菊
Owner 南京海澳斯生物医药科技有限公司
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