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Active medicine for lowering blood pressure and preparation method thereof

A kind of technology of pharmacy and prodrug, applied in the preparation of said medicine, the field of active medicine for lowering blood pressure

Inactive Publication Date: 2018-07-20
佳木斯大学附属第一医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although ACEI has many advantages, such as good and long-lasting antihypertensive effect, wide range of treatment, and small side effects, there are still some negative effects, such as dry cough, asthma, bone marrow suppression, and angioedema in some patients after taking it. , pruritus and eosinophilia and other adverse reactions

Method used

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  • Active medicine for lowering blood pressure and preparation method thereof
  • Active medicine for lowering blood pressure and preparation method thereof
  • Active medicine for lowering blood pressure and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1: 2-((1H-imidazol-1-yl)methyl)-N-(pyridin-4-yl)-3,4-dihydroquinoline-1(2H)-carboxamide (Compound 1) Synthesis

[0050]

[0051] Dissolve 10 mmol of 2-chloromethyl-1,2,3,4-tetrahydroquinoline in 100 ml of dichloromethane, add an equivalent amount of 4-isocyanato-pyridine, and stir at room temperature for 12 hours. Then dichloromethane was added to dilute the reaction solution, then 100ml of 2M hydrochloric acid was added, the organic layer was washed with 2M HCl, saturated sodium bicarbonate, saturated sodium chloride, and finally dried with anhydrous sodium sulfate, the solvent was removed under reduced pressure, and vacuum-dried to obtain The crude product was directly put into the next reaction without purification.

[0052] The above dried product was dissolved in 120ml THF, 20ml of 20mmol NaOH aqueous solution was added, and then a solution of 10mmol imidazole dissolved in 20ml THF was added dropwise, and the temperature was raised to reflux and stirred...

Embodiment 2

[0055] Example 2: 2-(2-Hydroxy-3-(1H-imidazol-1-yl)propyl)-N-(pyridin-4-yl)-3,4-dihydroquinoline-1(2H)- Synthesis of Formamide (Compound 2)

[0056]

[0057] Take 10mmol of 1-chloro-3-(1,2,3,4-tetrahydroquinolin-2-yl)propan-2-ol and dissolve it in 100ml of dichloromethane, add an equivalent amount of 4-isocyanic acid base-pyridine and stirred at room temperature for 10 hours. Then dichloromethane was added to dilute the reaction solution, then 100ml of 2M hydrochloric acid was added, the organic layer was washed with 2M HCl, saturated sodium bicarbonate, saturated sodium chloride, and finally dried with anhydrous sodium sulfate, the solvent was removed under reduced pressure, and vacuum-dried to obtain The crude product was directly put into the next reaction without purification.

[0058] The above dried product was dissolved in 100ml of ethanol, 20ml of 20mmol NaOH aqueous solution was added, and then a solution of 10mmol of imidazole dissolved in 20ml of ethanol was ad...

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PUM

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Abstract

The invention relates to an active medicine for lowering blood pressure. The medicine is an angiotensin converting enzyme (ACE) inhibitor. The invention also relates to a preparation method of the medicine. Shown by an in-vitro test result, a compound provided by the invention has favorable inhibitory activity to an ACE; the IC50 (half maximal inhibitory concentration) of the compound is 100nm orbelow. Shown by an animal test, the compound provided by the invention has an obvious blood sugar lowering effect on a spontaneously hypertensive rat, and the pressure lowering effect of the compoundis approximately equivalent to that of nitrendipine.

Description

technical field [0001] The invention relates to the field of medicines. In particular, the invention relates to an active medicine for lowering blood pressure. The medicine is an angiotensin-converting enzyme inhibitor, and the invention also relates to a preparation method of the medicine. Background technique [0002] Hypertension is the most common cardiovascular disease in my country, and its incidence rate is as high as 20% among adults. Because the arterial blood pressure of hypertensive patients is higher than normal blood pressure for a long time, it can not only cause symptoms such as headache, dizziness, and heart palpitations, but also cause patients Heart, brain, kidney and other organ damage can lead to hemorrhagic stroke, myocardial infarction, heart failure and cerebral thrombosis complications, leading to hemiplegia or death of the patient and significantly reducing the quality of life of the patient. The current common drugs for the treatment of hypertension ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/14C07D409/14C07D417/14A61K31/4709A61K31/506A61P9/12
CPCC07D401/14C07D409/14C07D417/14
Inventor 董天崴王爽石晶卢冬雪王敬磊
Owner 佳木斯大学附属第一医院
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