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Compound with antihypertensive activity and preparation method thereof

A compound and high blood pressure technology, applied in the field of biomedicine, can solve the problems of toxic and side effects of chemical drugs, chemical drug treatment can not meet expectations, etc., achieve the effect of cheap and easy to obtain reagents, mild reaction conditions, and reduce costs

Inactive Publication Date: 2015-04-29
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the different degrees of toxic and side effects of chemical drugs themselves, hypertension drugs with different mechanisms of action have different shortcomings, which often make the chemical drug treatment of hypertension fail to achieve the desired effect; and enhance the long-term effect of antihypertensive drugs Sex and stationarity are effective ways to improve the effect of antihypertensive drugs

Method used

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  • Compound with antihypertensive activity and preparation method thereof
  • Compound with antihypertensive activity and preparation method thereof
  • Compound with antihypertensive activity and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 9-[[α-[3-(2-ethyl)amino]propyl]-3,4-dimethoxy-α-(1-methylethyl)phenylacetonitrileoxy]-7H-furan [3,2-g]chromen-7-one and its hydrochloride, prepared by the following steps:

[0043] 1) Demethylation of compound A 8-methoxypsoralen by boron tribromide to obtain compound B xanthoxylin

[0044] Weigh 5.00g (24.75mmol) of 8-methoxypsoralen into a 250mL round-bottomed flask, stir and dissolve with 70mL of anhydrous dichloromethane, under nitrogen protection, stir for 10min under ice-salt bath conditions, and dissolve 13mL of three Dilute the boron bromide (2N) solution into 20mL of anhydrous dichloromethane, and then slowly add it dropwise into the dissolved 8-methoxypsoralen solution in the dark, the dropping time is controlled at 20min, and then placed at room temperature After reacting for 6 hours, neutralize with alkaline solution after the reaction, then filter and dry to obtain 4.30 g (21.29 mmol) of white solid powder with a yield of 92.1%.

[0045] Its phy...

Embodiment 2

[0064] Example 2 9-[[α-[3-(2-ethyl)amino]propyl]-3,4-dimethoxy-α-(1-methylethyl)phenylacetonitrileoxy]-7H-furan [3,2-g]chromen-7-one and its sulfate, prepared by:

[0065] Step 1) to step 6) are the same as in Example 1, that is, from compound A 8-methoxypsoralen to compound ① 9-[[α-[3-(2-ethyl)amino]propyl]-3 , The preparation steps of 4-dimethoxy-α-(1-methylethyl) phenylacetonitrile oxy]-7H-fur[3,2-g]chromen-7-one are the same; compound ③9-[[α -[3-(2-Ethyl)amino]propyl]-3,4-dimethoxy-α-(1-methylethyl)phenylacetonitrileoxy]-7H-furano[3,2-g]color The preparation of en-7-one sulfate, specifically:

[0066] 7) Compound ①9-[[α-[3-(2-ethyl)amino]propyl]-3,4-dimethoxy-α-(1-methylethyl)phenylacetonitrileoxy]-7H-furan [3,2-g] Chromene-7-one reacts with sulfuric acid to obtain compound ③ 9-[[α-[3-(2-ethyl)amino]propyl]-3,4-dimethoxy-α- (1-Methylethyl)phenylacetonitrileoxy]-7H-furo[3,2-g]chromen-7-one sulfate

[0067] Weigh 4.00g (7.94mmol) of 9-[[α-[3-(2-ethyl)amino]propyl]-3,4-d...

Embodiment 3

[0069] Example 3 9-[[α-[3-(2-ethyl)amino]propyl]-3,4-dimethoxy-α-(1-methylethyl)phenylacetonitrileoxy]-7H-furan [3,2-g]chromen-7-one (OW1) relaxes mesenteric artery in rats

[0070] Male SD rats (body weight 200-300 g, Experimental Animal Center, Xi'an Jiaotong University Medical College) were killed by neck dislocation, and the secondary branches of the mesenteric artery (MA) were taken out and placed in pre-cooled Krebs solution (composition (g / L): 6.954 NaCl, 0.343KCl, 1.260NaHCO3, 0.187NaH2PO4·2H2O, 0.166CaCl2, 0.244MgCl2·6H2O, 1.090 glucose, PH=7.2~7.4), and make a vascular ring specimen with a length of 3 mm. The vascular ring specimens were connected with a DMT vascular tension measurement system (Danish Myo Technology AIS Inc. 610M) with thin steel wires to record changes in vascular tension. The vascular ring specimens were balanced in Krebs solution saturated with 95% oxygen 5% carbon dioxide gas mixture at 37°C, and adjusted to zero until the vascular tension did n...

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Abstract

The invention discloses a compound with antihypertensive activity and a preparation method thereof. The compound has the property similar to that of imperatorin, displays the activity of diastole in research of in vitro vascular ring tension, and can be applied to preparation of an antihypertensive medicine. The preparation method of the compound with antihypertensive activity provided by the invention has the advantages of available material source, mild reaction condition, simple reaction process operation and inexpensive and available used reagent.

Description

technical field [0001] The invention relates to the technical field of biomedicine, and relates to a compound with antihypertensive activity and a preparation method thereof. Background technique [0002] Hypertension is currently one of the major diseases that seriously affect human health and threaten human life. It is the most common cardiovascular disease and is closely related to myocardial infarction, stroke, coronary heart disease, heart failure, and renal failure. Nearly 3 million people die from cardiovascular and cerebrovascular diseases in our country every year, accounting for 51% of the total death causes in our country every year; and 75% of the surviving patients lose their ability to work to varying degrees, and 40% of them are seriously disabled. Cardiovascular disease has become the number one killer of human beings. The key to preventing and treating cardiovascular and cerebrovascular diseases is the prevention and treatment of hypertension. [0003] Acc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/04A61K31/37A61P9/12
Inventor 贺浪冲张杰周楠贺建宇王涛贺怀贞王程卢闻
Owner XI AN JIAOTONG UNIV
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