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

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

Inactive Publication Date: 2016-02-24
NANJING UNIV
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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 drugs for preventing or treating pancreatic fibrosis
  • Composition and application thereof in drugs for preventing or treating pancreatic fibrosis
  • Composition and application thereof in drugs for preventing or treating pancreatic fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] The preparation of embodiment 1 compound Schiglautone A

[0011] The preparation method of the compound Schiglautone A (I) refers to the method published by Fan-Yu Mengetal.

[0012]

Embodiment 2

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

[0014] 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

[0019] The synthesis of O-(tetrahydropyrrolyl) ethyl derivative (III) of embodiment 3 Schiglautone A

[0020] Compound II (358 mg, 0.5 mmol) was dissolved in 15 mL of acetonitrile, anhydrous potassium carbonate (690 mg, 5.0 mmol), potassium iodide (168 mg, 1.0 mmol) and pyrrolidine (2840 mg, 40 mmol) were added thereto, and the mixture was heated to reflux for 6 h. After the reaction, the reaction solution was poured into ice water, extracted 4 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 a brown powder of compound III (21...

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Abstract

The invention relates to the field of organic synthesis and pharmaceutical chemistry, in particular to a composition 82092202050618, a preparation method and use of the composition 82092202050618 in preparation of drugs for preventing or treating pancreatic fibrosis. The invention discloses a composition 82092202050618 and a preparation method thereof. A pharmacology experiment shows that the composition 82092202050618 has an effect of preventing or treating pancreatic fibrosis, and has value of development of the drugs for preventing or treating pancreatic fibrosis.

Description

technical field [0001] The present invention relates to the fields of organic synthesis and medicinal chemistry, in particular to composition 82092202050618, a preparation method and its application. 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 co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K31/4025A61P1/18C07D295/088
CPCA61K31/4025A61K31/496C07D295/088A61K2300/00
Inventor 吴俊华黄蓉王慧
Owner NANJING UNIV
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