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Composition and application thereof to medicines 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 high toxicity and low safety

Inactive Publication Date: 2016-01-20
苏州贺澳德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 to medicines for preventing or treating pancreatic fibrosis
  • Composition and application thereof to medicines for preventing or treating pancreatic fibrosis
  • Composition and application thereof to medicines for preventing or treating pancreatic fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] The preparation of embodiment 1 compound PsiguadialA

[0011] The preparation method of the compound PsiguadialA (I) refers to the method published by Meng Shao et al. (Meng Shao et al., 2010. Psiguadials A and B, Two Novel Meroterpenoids with Unusual Skeletons from the Leaves of Psidiumguajava. Organic Letters 12 (2010) 5040-5043).

[0012]

Embodiment 2

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

[0014] Compound I (474 ​​mg, 1.00 mmol) was dissolved in 20 mL of benzene, tetrabutylammonium bromide (TBAB) (0.16 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 12 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=100:0.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (502mg, 73%) . ...

Embodiment 3

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

[0020] Compound II (344 mg, 0.5 mmol) was dissolved in 20 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 yellow concentrated elution band was collected and the solvent was evaporated to obtain a yellow powder of compound III (...

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Abstract

The invention relates to the field of organic synthesis and medicinal chemistry and in particular relates to a composition, a preparation method and an application of the composition to preparation of medicines for preventing or treating pancreatic fibrosis. The invention discloses the composition and the preparation method thereof. Pharmacological experiments show that the composition has the function of preventing or treating pancreatic fibrosis and has the value in developing the medicines for preventing or treating 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): A61K31/5377A61P1/18A61K31/4025
Inventor 朱磊磊
Owner 苏州贺澳德生物医药科技有限公司
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