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Preparation method and application of pyranoindole compound

A technology of pyranoindoles and compounds, which is applied in the field of heterocyclic compounds to achieve the effects of low in vivo toxicity, improved plasminogen activity and low blood risk

Active Publication Date: 2019-04-16
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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  • Preparation method and application of pyranoindole compound
  • Preparation method and application of pyranoindole compound
  • Preparation method and application of pyranoindole compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Inoculate the strain FG216 on the slant medium, and then inoculate the seed culture solution of the cultured slant strain FG216 in the Chase 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 filtered and discarded, 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-acetic acid, the volume ratio was 7...

Embodiment 2

[0058] Take 1 mg of the two pyranoindole compounds of structural formula I and II prepared in Example 1, dissolve them in 0.5 mL of DMSO, add water for injection as usual, fine filter, potting and sterilize to prepare Injection.

Embodiment 3

[0060] With the two pyranoindole compounds of structural formula I and II 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 , stirred to dissolve, filtered with a sterile suction filter funnel, divided into ampoule bottles, freeze-dried at low temperature and sealed aseptically to obtain a powder injection.

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Abstract

The invention relates to a preparation method and application of a pyrane diindole compound. The pyrane diindole compounds are chiral compounds, and the structural formulae of the pyrane diindole compounds are I and II. The preparation method comprises the following steps: inoculating an FG216 bacterial strain in an inclined medium; then, inoculating the inclined bacterial strain FG216 seed culture liquid in a Czapek-Dox medium according to the inoculating amount of 1 percent; culturing on a constant-temperature shaking table, and extracting with methyl alcohol; and performing centrifugal treatment, concentrating under reduced pressure, performing vacuum and finally performing acetoxylation to obtain the pyrane diindole compound after a dried solid is subjected to silica gel chromatography. The two pyrane diindole compounds have certain thrombolysis activity in vitro; EC50 are respectively 40 [mu]M and 120 [mu]M; the compound II has extremely low in-vivo toxicity, has certain thrombolysis activity and has a reasonable half-life period. The compound has the pharmacodynamic characteristics of low bleeding risk, no damage to blood factor and clear target spot, and can be used for a medicament for treating or preventing a thromboembolic disease.

Description

technical field [0001] The present invention relates to heterocyclic compounds, in particular to a preparation method and application of a pyranoindole compound. Background technique [0002] Thrombotic disease is one of the three major diseases that cause human death, which seriously threatens human life and health. The number of deaths caused by thrombotic disease 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 potential active plasminogen in the blood to form active plasmin to degrade thrombus fibrin degradation products and dissolve thrombus. . Fibrinolytic therapy is known as one of the top ten discoveries in the field of cardiovascular and cerebrovascular pharmacology in the 20th century. [0003] There are nea...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D491/052A61K31/454A61P7/02
CPCC07D491/052
Inventor 吴文惠郭锐华姜胜男段东包斌周文靖
Owner SHANGHAI OCEAN UNIV
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