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Preparation method and application of anti-stroke aspirin twin drug based on TXA2 (thromboxane A2)/ROS double targets

A technology for aspirin and cerebral apoplexy, applied in the direction of antidote, drug combination, blood disease, etc., can solve problems such as renal abnormalities, and achieve the effect of easy application, easy preparation and quality control, and simple structure

Inactive Publication Date: 2017-11-28
KANGDA COLLEGE OF NANJING MEDICAL UNIV
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  • Abstract
  • Description
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Problems solved by technology

However, Edaravone is prone to side effects such as liver and kidney abnormalities

Method used

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  • Preparation method and application of anti-stroke aspirin twin drug based on TXA2 (thromboxane A2)/ROS double targets
  • Preparation method and application of anti-stroke aspirin twin drug based on TXA2 (thromboxane A2)/ROS double targets
  • Preparation method and application of anti-stroke aspirin twin drug based on TXA2 (thromboxane A2)/ROS double targets

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Embodiment Construction

[0021] The following examples can enable those skilled in the art to understand the present invention more fully, but do not limit the present invention in any way.

[0022] Synthetic route of the present invention:

[0023]

[0024] Aspirin (35mmol) and thionyl chloride (3ml, 42mmol) were mixed and azeotropically refluxed to prepare acetylsalicyloyl chloride, diluted with dichloromethane (10-20ml) for later use; at a suitable temperature, an appropriate amount of Edaravone (5.5 g, 32mmol) was dissolved in dichloromethane (50ml~100ml), triethylamine (5ml, 32mmol) was added dropwise, after stirring for 0.5~1h, acetylsalicyloyl chloride was added dropwise into the above reaction system, and the temperature of the reaction system was controlled , stirred for 1-2 hours, added 200-300ml of ethyl acetate to extract, washed three times with water, washed three times with saturated sodium bicarbonate, washed three times with saturated sodium chloride solution, dried over anhydrous ...

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Abstract

The invention provides a preparation method and an application of an anti-stroke aspirin twin drug based on TXA2 (thromboxane A2) / ROS double targets. Aspirin and edaravone are linked through ester bonds to form the twin drug, and the specific structure is shown as (I). The twin drug probably has double mechanisms, has stronger effects of eliminating ROS, protecting cranial nerves and improving brain functions while having an anti-TXA2 function, anti-platelet aggregation and cranial nerve protection can be combined organically, and a novel idea is provided for research and development of stroke treatment drugs.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a preparation method of a TXA2 / ROS dual-target anti-stroke aspirin drug pair, and an application of the drug pair as a drug for treating cerebral apoplexy. Background technique [0002] Stroke, also known as stroke or cerebrovascular accident, is an acute cerebrovascular disease with sudden onset and common features of focal neurological deficits, including cerebral hemorrhage, subarachnoid hemorrhage, and cerebral infarction. The most common cause is blood coagulation to form blood clots, blocking the blood vessels in the brain, resulting in local brain tissue ischemia, hypoxia, encephalomalacia, and necrosis, which is a clinically intractable disease. The most important causes are hypertension, cerebral arteriosclerosis, acute hypotension, arteritis, blood diseases, trauma, etc., but hypertension and atherosclerosis are the most important. Stroke is one of the three major causes of human...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D231/22A61P25/00A61P7/02A61P9/10A61P39/06
Inventor 李洪雷马少杰储振飞顾兴猛江冉孙玲玲
Owner KANGDA COLLEGE OF NANJING MEDICAL UNIV
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