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Composition and application of composition to acute renal failure resisting drugs

A technology of acute renal failure and composition, applied in the direction of drug combination, peptide/protein composition, urinary system diseases, etc., to achieve the effect of improving function

Inactive Publication Date: 2016-01-27
CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are few clinical drugs that have obvious effects on improving renal blood perfusion disorder and reducing renal tissue damage

Method used

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  • Composition and application of composition to acute renal failure resisting drugs
  • Composition and application of composition to acute renal failure resisting drugs
  • Composition and application of composition to acute renal failure resisting drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1 Preparation of compound Schiglautone A

[0013] The preparation method of the compound Schiglautone A(I) refers to the method published by Fan-YuMeng et al. (Fan-YuMengetal., 2011.SchiglautoneA, aNewTricyclicTriterpenoidwithaUnique6 / 7 / 9-FusedSkeletonfromtheStemsofSchisandraglaucescens.Organic Letters 13 (2011) 1502–1505

[0014]

Embodiment 2

[0015] Example 2 Synthesis of O-Bromoethyl Derivative (II) of Schiglautone A

[0016] Compound I (502mg, 1.00mmol) was dissolved in 15mL of benzene, tetrabutylammonium bromide (TBAB) (0.08g), 1,2-dibromoethane (7.520g, 40.00mmol) and 6mL of benzene were added to the solution 50% sodium hydroxide solution. The mixture was stirred at 35 degrees Celsius for 8 hours. After 8h, the reaction solution was poured into ice water, immediately extracted twice with dichloromethane, and the organic phase solutions were combined. Then the organic phase solution was washed 3 times with water and saturated brine in turn, and then dried over anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain the 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 the brown powder of co...

Embodiment 3

[0021] Example 3 Synthesis of O-(Diethylamino)ethyl Derivative (III) of Schiglautone A

[0022] Compound II (358mg, 0.5mmol) was dissolved in 10mL of acetonitrile, anhydrous potassium carbonate (690mg, 5.0mmol), potassium iodide (168mg, 1.0mmol) and diethylamine (2920mg, 40mmol) were added to it, and the mixture was heated to reflux for 8h . After the reaction, the reaction solution was poured into ice water, extracted twice with the same amount of dichloromethane, and the organic phases were combined. The combined organic phase was washed with water and saturated brine in turn, 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=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain the brown powder of compound III (231.2mg, 66% ).

[0023] 1 HNMR(500...

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PUM

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Abstract

The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method and application of the composition to preparation of acute renal failure resisting drugs. Through pharmacological experiments, the composition is capable of resisting acute renal failure and has acute renal failure resisting drug development value.

Description

Technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to compositions, preparation methods and uses thereof. Background technique [0002] Acute Renal Failure (AcuteRenalFailure, ARF) is a clinical syndrome caused by a variety of reasons. It can be seen in patients in various clinical departments. The incidence is high and often brings serious consequences. It is characterized by the short-term (hours to days) kidney The function drops sharply, and the clinical manifestations are acute oliguria (urine volume <400mLPd) or anuria (urine volume <100mLPd), the excretion of nitrogen metabolites in the body is impeded, azotemia occurs rapidly, water, electrolyte, and acid-base balance are disturbed, and the corresponding dysfunction of various systems in the body is caused. The main factors that cause acute renal failure are the rapid reduction of renal blood flow, as well as the oxidative stress and cell damage cau...

Claims

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Application Information

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IPC IPC(8): A61K31/195A61P13/12C07C217/12
Inventor 华子春吴俊华黄蓉王慧
Owner CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
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