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Pyran indole compounds as well as preparation method and application thereof

A technology for pyranoindole and compounds, which is applied in the field of pyranoindole compounds and their preparation, can solve the problem of low blood risk and achieve the effects of low blood risk, accelerated degradation, and high specificity

Inactive Publication Date: 2015-12-16
SHANGHAI OCEAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] To sum up, there is a very large market demand for drugs for the treatment of thrombosis, but there are generally safety problems in clinically used drugs for the treatment of thrombosis. The emergence of small molecular compounds with high specificity as drugs, and develop them into efficient, specific and safe thrombolytic drugs

Method used

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  • Pyran indole compounds as well as preparation method and application thereof
  • Pyran indole compounds as well as preparation method and application thereof
  • Pyran indole compounds as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Inoculate the strain FG216 on the slant medium, and then inoculate the cultivated slant strain FG216 seed culture solution in the Chase medium according to the inoculation 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 Erlenmeyer 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 obtained dry solid was subjected to silica gel column chromatography with chloroform-methanol (5:1, v / v) to obtain A p...

Embodiment 2

[0053] Take 1 mg of the two pyranoindole compounds in the structural formula I prepared in Example 1 and dissolve them in 0.5 mL of DMSO, add water for injection as usual, fine filter, seal and sterilize to make injection liquid.

Embodiment 3

[0055] With the two pyranoindole compounds in the structural formula I prepared in Example 1, take 1 mg each and dissolve them in 0.5 mL of DMSO, add water for injection as usual, and dissolve it in sterile water for injection, Stir to dissolve, filter with a sterile suction filter funnel, pack in ampoules, lyophilize at low temperature, and aseptically melt seal to obtain a powder injection.

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Abstract

The invention relates to a heterocyclic compound, in particular to pyran indole compounds as well as a preparation method and an application thereof. The pyran indole compounds are chiral compounds; the preparation method comprises steps as follows: FG216 strains separated from seas of Zhoushan islands are inoculated to a slant culture medium, then, a seed culture solution of slant strains FG216 is inoculated to a Czapek-Dox medium according to the inoculation amount of 1%, cultured on a constant-temperature shaking table and extracted with methanol; centrifugation, concentration under reduced pressure and vacuum drying are performed, and finally, dried substances are subjected to silica-gel column chromatography. The pyran indole compounds can improve the activity of plasminogen and promote decomposition of fluorescein isothiocyanate-fibrous protein, has certain thrombolysis activity, can be used in drugs for treating or preventing thromboembolic diseases, has low blood danger, doesn't damage blood factors and is high in specificity.

Description

Technical field [0001] The present invention relates to heterocyclic compounds, in particular to a pyrano-indole compound and its preparation method and application. Background technique [0002] Thromboembolic disease is one of the three major causes of death in humans and seriously threatens human life and health. There are currently about 15 million patients worldwide, and the number of deaths caused by it has exceeded that of malignant tumors. Thrombolytic therapy is an effective treatment for early acute myocardial infarction and other thromboembolic diseases. Fibrinolytic therapy is an effective treatment for early acute myocardial infarction and other thromboembolic diseases. It mainly activates the potentially active plasminogen in the blood through drugs. , forming active plasmin to degrade thrombus into fibrin degradation products, dissolving the thrombus, and achieving the therapeutic purpose of fibrinolytic therapy. Fibrinolytic therapy is hailed as one of the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/18C12P17/18A61K31/403A61P7/02C12R1/29
CPCA61K9/0019A61K9/0053A61K9/08A61K9/14A61K9/19A61K9/4866A61K47/36C07D491/18C12P17/182
Inventor 郭锐华吴文惠包斌张依婷王格张朝燕
Owner SHANGHAI OCEAN UNIV
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