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Composition and application thereof in preparation of drugs for treating or preventing renal fibrosis

A technology for renal fibrosis and renal interstitial fibrosis, applied in drug combinations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of low safety and high toxicity, and achieve good anti-renal fibrosis Effect

Inactive Publication Date: 2016-03-23
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 renal fibrosis 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 with high efficiency and low toxicity

Method used

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  • Composition and application thereof in preparation of drugs for treating or preventing renal fibrosis
  • Composition and application thereof in preparation of drugs for treating or preventing renal fibrosis
  • Composition and application thereof in preparation of drugs for treating or preventing renal fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] The preparation of embodiment 1 compound Schiglautone A

[0012] The preparation method of the compound Schiglautone A (I) refers to the method published by Fan-Yu Mengetal.

[0013]

Embodiment 2

[0014] The synthesis of the O-bromoethyl derivative (II) of embodiment 2SchiglautoneA

[0015] 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

[0020] Synthesis of O-(morpholinyl) ethyl derivative (III) of embodiment 3 Schiglautone A

[0021] 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 fields of organic synthesis and pharmaceutical chemistry, and specifically relates to a composition, a preparation method, and an application thereof in the preparation of drugs for treating or preventing renal fibrosis. The invention discloses a composition and a preparation method thereof. The pharmacology experiment results show that the provided composition can prevent or treat renal fibrosis, and can be used to develop drugs for preventing or treating renal 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] Renal fibrosis (including renal interstitial fibrosis and glomerulosclerosis) is the main pathological basis of the final stage of renal damage caused by various reasons. Proliferation and activation of stromal cells are related to the imbalance of vasoactive substances, cytokines and extracellular matrix transformation. Renal interstitial fibrosis is almost a common path for all primary or secondary renal diseases to progress to end-stage renal failure. It is urgent to develop anti-renal fibrosis drugs with high efficiency and low toxicity. [0003] The existing drugs for the treatment of renal fibrosis 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 modif...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61K31/195A61P13/12
CPCA61K9/4866A61K31/195A61K31/5377A61K2300/00
Inventor 吴俊华周未末
Owner NANJING UNIV
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