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Pyranoindole acetylation derivative, and preparation method and application thereof

A technology of pyrazolindole acetyl and pyrazolindole acetyl is applied in the field of pyrazolindole acetylated derivatives and preparation thereof, and achieves the effects of high specificity, low bleeding risk and promoting degradation

Inactive Publication Date: 2017-07-14
SHANGHAI OCEAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Typical fibrinolytic therapy clinically used drugs such as tissue-type plasminogen activator, urokinase-type plasminogen activator, etc. will bring a significant risk of bleeding and can only be used to treat patients with severe thrombosis

Method used

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  • Pyranoindole acetylation derivative, and preparation method and application thereof
  • Pyranoindole acetylation derivative, and preparation method and application thereof
  • Pyranoindole acetylation derivative, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Activate the strain FG216 in the slant medium, and then inoculate the cultivated slant strain FG216 seed culture solution in the above medium according to the inoculum amount of 1%, at 25°C, 180r min -1 Cultivate on a constant temperature shaker for 4 days, then add 1% ornithine by weight in the volume of the medium, and cultivate for 24 hours to complete the fermentation culture. After the cultivation, add an equal volume of methanol to the flask, sonicate for 15 minutes, centrifuge at 10,000 rpm for 15 minutes, discard the precipitate, evaporate the supernatant to dryness under reduced pressure at 60°C, and dry the concentrate for 8 hours in vacuum. The solid was dissolved in 20 mL of methanol solution, the precipitate was discarded by filtration, the supernatant was collected, concentrated under reduced pressure and dried in vacuo, the resulting dried solid was subjected to silica gel column chromatography chloroform-methanol-formic acid (7:1:0.1, v / v ), and obtain t...

Embodiment 2

[0044] The pyranoindole acetylated derivatives obtained in Example 1 were taken, 1 mg each was dissolved in 0.5 mL of DMSO, and water for injection was added as usual, finely filtered, potted and sterilized to make an injection.

Embodiment 3

[0046] The acetylated derivatives of pyranoindole obtained in Example 1, 1 mg each was dissolved in 0.5 mL of DMSO, and water for injection was added as usual, dissolved in sterile water for injection, stirred to dissolve, and used Filter with a sterile suction filter funnel, pack in ampoules, freeze-dry at low temperature, and then aseptically melt seal to obtain a powder for injection.

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Abstract

The invention relates to a heterocyclic compound, and especially relates to a pyranoindole acetylation derivative, and a preparation method and an application thereof. The pyranoindole acetylation derivative is 2,5-di((2-(2,6-dimethyl-2,6-diene)nonyl)-(2-methyl-3-acetoxy)-pyrano(5-acetoxy)isoindolinone)-pentanoic acid, and has structural formula I. The preparation method comprises the following steps: inoculating a slant medium with an FG216 strain, inoculating a Czapek-Dox medium with the obtained slant strain FG216 seed culture liquid according to an inoculation amount of 1%, carrying out culture on a constant temperature shaking tablet, and carrying out methanol extraction; and carrying out centrifugation, reduced pressure concentration and vacuum drying, carrying out dry solid substance silica gel column chromatography, and carrying out acetylation to prepare the pyranoindole acetylation derivative. The plasminogen activity of the pyranoindole acetylation derivative I is improved by 3.5 times or above, and the pyranoindole acetylation derivative has certain thrombolysis activity. The above compound has the characteristics of small hemorrhage danger, no damages to blood factors, and clear medicine effects of the target, and can be used in medicines for treating or preventing thromboembolic diseases.

Description

Technical field [0001] The present invention relates to heterocyclic compounds, in particular to a pyranyl indole acetylated derivative and its preparation method and application. Background technique [0002] Thrombotic diseases are one of the three major causes of human death and seriously threaten human life and health. The number of deaths caused by thrombotic diseases has exceeded that of malignant tumors. Thrombolytic therapy is an effective treatment for early acute myocardial infarction and thromboembolic disease. Fibrinolytic therapy is an effective treatment for early acute myocardial infarction and other thrombotic diseases. This therapy uses drugs to activate the potentially active plasminogen in the blood, forming active plasmin to degrade the thrombus into fibrin degradation products to dissolve the thrombus. . Fibrinolytic therapy is hailed as one of the top ten discoveries in the field of cardiovascular and cerebrovascular pharmacology in the 20th century. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/00A61K31/407A61P7/02C12P17/18C12R1/29
CPCC07D519/00C12P17/18
Inventor 郭锐华段东钱士云张依婷王格包斌吴文惠
Owner SHANGHAI OCEAN UNIV
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