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A kind of furanocoumarin compound and its preparation method and application

A technology of furanocoumarin and its use, which is applied in the field of biomedicine, can solve the problems of toxic and side effects of chemical drugs, unexpectable chemical drug treatment of hypertension, drug resistance of antihypertensive drugs, etc., and achieve cheap and easy to obtain reagents, Mild reaction conditions, lower systolic and diastolic blood pressure

Active Publication Date: 2021-03-23
YANBIAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although there are many types of antihypertensive drugs in clinical use and various mechanisms of action, due to the different degrees of toxic and side effects of chemical drugs, hypertension drugs with different mechanisms of action have different shortcomings, and antihypertensive drugs with a single mechanism of action often produce Drug resistance, which often prevents chemotherapeutic treatment of hypertension from achieving the desired effect

Method used

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  • A kind of furanocoumarin compound and its preparation method and application
  • A kind of furanocoumarin compound and its preparation method and application
  • A kind of furanocoumarin compound and its preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] 1) Stir the dichloromethane solution of chlorosulfonic acid (100 mmol / 20 mL) in an ice bath for 30 min, slowly add xanthotoxin (10 mmol) in batches, and continue the ice bath for 1 h;

[0024] 2) After the reaction was completed, the solvent was removed under reduced pressure, and then slowly added dropwise to the ice-water mixture, filtered with suction, washed, and dried to obtain the white chlorosulfonated product of xanthotoxin;

[0025] 3) Dissolve 5-aminotetrazole (1 mmol) and N,N-diisopropylethylamine (2 mmol) in 10 mL of dichloromethane under an ice bath;

[0026] 4) After cooling down for 30 minutes, add the chlorosulfonated pepper toxin (0.8 mmol) prepared in step 2), continue the reaction for 2 hours, add water for extraction, wash with 10% hydrochloric acid, saturated sodium bicarbonate and saturated saline successively, and filter with suction , drying, column chromatography to obtain compound S31; named as:

[0027] 9-methoxy-7-oxo-N-(1 H -tetrazol-5-yl)...

Embodiment 2

[0030] pharmaceutical composition

[0031] Formulation for 1000 tablets each containing 100 mg of active ingredient:

[0032] Compound S31-----------------------------------100 g

[0033] Hydroxypropyl cellulose ----------------------------- 2 g

[0034] Wheat starch ----------------------------------- 10 g

[0035] Lactose --------------------------------------- 100 g

[0036] Magnesium stearate -------------------------------------- 3 g

[0037] Talc --------------------------------------- 3 g

[0038] The dosage used should be adapted to the nature and severity of the disease, the route of administration and the age and weight of the patient. The daily dose varies between 0.1 mg-1.0 g, and can be administered once or several times.

[0039] Further prove the medical purposes of compound of the present invention by following test:

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Abstract

The invention discloses a furocoumarin compound, and a preparation method and medical application thereof. The furocoumarin compound is a novel compound having vasodilating activity; and the compoundis obtained by structurally modifying and optimizing the natural product xanthotoxin to improve its physical and chemical properties, pharmacological activity and drug-forming properties. The preparation method for the furocoumarin compound provided by the invention has the advantages that raw materials are widely available, reaction conditions are mild, reaction process is simple to operate and reagents used therein are cheap and easily available. The prepared novel furocoumarin compound has effect similar to the effect of xanthotoxin; the study results of isolated vascular ring tension indicate that the relaxation effect of the novel furocoumarin compound on the aortic vessels of rat is stronger than the relaxation effect of xanthotoxin and the positive control drug nifedipine; the cytotoxicity of the novel furocoumarin compound on normal liver cells L02 in vitro is significantly lower than the cytotoxicity of nifedipine; and the results of in-vivo antihypertensive studies show thatthe antihypertensive effect of the novel furocoumarin compound is stronger than the antihypertensive effect of xanthotoxin and nifedipine, so the novel furocoumarin compound can be applied to the preparation of antihypertensive drugs.

Description

technical field [0001] The invention discloses a furinocoumarin compound, which is a new compound; the invention also provides a preparation method and medical application of the furanocoumarin compound, belonging to the technical field of biomedicine. Background technique [0002] Cardiovascular and cerebrovascular diseases have become the number one killer of human health, and hypertension is one of the important causes of cardiovascular and cerebrovascular diseases. At present, according to the report of the World Health Organization, the incidence of hypertension in the world population has exceeded 10%, and the number of hypertensive patients in my country has exceeded 100 million. With the increasing aging of our population, the number of hypertensive patients will further increase. [0003] Although there are many types of antihypertensive drugs in clinical use and various mechanisms of action, due to the different degrees of toxic and side effects of chemical drugs, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/04A61K31/41A61P9/12A61P9/08
CPCA61P9/08A61P9/12C07D493/04
Inventor 全哲山曹丽华沈庆坤尹秀梅王思宏
Owner YANBIAN UNIV
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