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Application of composition of O-(diethylamino)ethyl derivative and O-(piperazinyl)ethyl derivative of Harrisotone A in pancreatic fibrosis preventing or treating drugs

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 high toxicity and low safety

Inactive Publication Date: 2017-02-22
NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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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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  • Application of composition of O-(diethylamino)ethyl derivative and O-(piperazinyl)ethyl derivative of Harrisotone A in pancreatic fibrosis preventing or treating drugs
  • Application of composition of O-(diethylamino)ethyl derivative and O-(piperazinyl)ethyl derivative of Harrisotone A in pancreatic fibrosis preventing or treating drugs
  • Application of composition of O-(diethylamino)ethyl derivative and O-(piperazinyl)ethyl derivative of Harrisotone A in pancreatic fibrosis preventing or treating drugs

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Experimental program
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Effect test

Embodiment 1

[0010] The preparation of embodiment 1 compound Harrisotone A

[0011] 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.

[0012]

Embodiment 2

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

[0014] 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

[0018] The synthesis of the O-(diethylamino) ethyl derivative (III) of embodiment 3 Harrisotone A

[0019] Compound II (396mg, 0.5mmol) was dissolved in 15mL of acetonitrile, anhydrous potassium carbonate (345mg, 2.5mmol), potassium iodide (84mg, 0.5mmol) and diethylamine (2920mg, 40mmol) were added thereto, and the mixture was heated to reflux for 3h . After the reaction, the reaction solution was poured into 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=100:1.5, v / v), and the concentrated brown elution band was collected and concentrated to give Compound III as a pale yellow solid (246.1mg, 64%) .

[0...

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Abstract

The invention relates to the field of organic synthesis and medicinal chemistry and particularly relates to a composition, a preparation method and an application of the composition in preparing pancreatic fibrosis preventing or treating drugs. The invention discloses the composition and the preparation method thereof. Pharmacological experiments indicate that the composition provided by the invention has an effect of preventing or treating pancreatic fibrosis and a value in developing pancreatic fibrosis preventing or treating 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] 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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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/495A61K31/132A61P1/18
CPCA61K31/495A61K31/132A61K2300/00
Inventor 陆贤
Owner NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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