The-GRPAKRGDV decapeptide, and preparation method, activities and application thereof

A technology of -z-lys and -asp-obzl, applied in the preparation and treatment of ischemic stroke, the active field of treatment of ischemic stroke, can solve the problems of thrombolytic drug bleeding, reperfusion injury, reembolization, etc.

Active Publication Date: 2017-01-11
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Existing thrombolytic drugs have problems such as bleeding, reembolization, and reperfusion injury, so finding new anti-ischemic stroke drugs has important application value

Method used

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  • The-GRPAKRGDV decapeptide, and preparation method, activities and application thereof
  • The-GRPAKRGDV decapeptide, and preparation method, activities and application thereof
  • The-GRPAKRGDV decapeptide, and preparation method, activities and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 prepares Boc-Ala-Lys(Z)-OBzl(1)

[0029] Dissolve 2.08g (11mmol) Boc-Ala in 20mL anhydrous tetrahydrofuran (THF), add 1.35g (10mmol) 1-hydroxybenzotriazole (HOBt) and 2.47g (12mmol) dissolved in anhydrous THF under ice cooling Dicyclohexylcarbonyldiimide (DCC) was stirred for 0.5 hour to obtain reaction solution A. After 30 minutes, 4.07g (10mmol) HCl Lys(Z)-OBzl was dissolved in 15mL THF, and the pH was adjusted to 9 with N-methylmorpholine, then added to the reaction solution A, stirred at room temperature for 12 hours, TLC (Developer CHCl 3 :MeOH=30:1) showed that HCl·Lys(Z)-OBzl disappeared. The dicyclohexylurea (DCU) in the reaction solution was removed by filtration, the reaction solution was concentrated to dryness under reduced pressure, the residue was dissolved in 100 mL of ethyl acetate, and the insoluble matter was filtered off. The filtrate was successively washed 3 times with saturated aqueous sodium bicarbonate solution, 3 times with 5% aq...

Embodiment 2

[0030] Example 2 Preparation of HCl Ala-Lys(Z)-OBzl(2)

[0031] Dissolve 2.0g (3.7mmol) Boc-Ala-Lys(Z)-OBzl in a small amount of dry ethyl acetate, add 20mL of 4N hydrogen chloride-ethyl acetate solution under ice-salt bath, react under ice-cooling for 4 hours, TLC (CHCl 3 :MeOH, 30:1) showed that the raw material point disappeared and the reaction was complete. The reaction solution was concentrated under reduced pressure, and the residue was dissolved in ethyl acetate and concentrated under reduced pressure. This operation was repeated three times to remove free hydrogen chloride, and the residue was washed three times with anhydrous ether to obtain 1.6 g (90%) of the title compound as a colorless powder. ESI-MS(m / z): 442[M+H] + .

Embodiment 3

[0032] Embodiment 3 prepares Boc-Pro-Ala-Lys(Z)-OBzl(3)

[0033] Using the method of Example 1, 1.7 g (78%) of the title compound was obtained as a yellowish oil from 731 mg (3.4 mmol) of Boc-Pro and 1.8 g (3.3 mmol) of HCl·Ala-Lys(Z)-OBzl. ESI-MS(m / z): 639[M+H] + .

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Abstract

The invention discloses a The-Gly-Arg-Pro-Ala-Lys-Arg-Gly-Asp-Val decapeptide, a preparation method thereof, and an ischemic apoplexy treatment activity, an antithrombotic activity and a thrombus dissolving activity of the decapeptide. The invention also discloses an application of the decapeptide in the preparation of ischemic apoplexy treatment, antithrombosis and thrombus dissolving medicines.

Description

technical field [0001] The present invention relates to The-Gly-Arg-Pro-Ala-Lys-Arg-Gly-Asp-Val decapeptide, to its preparation method, to its activity for treating ischemic stroke, antithrombotic activity and thrombolytic activity. Therefore, the present invention relates to its application in the preparation of antithrombotic and thrombolytic drugs for treating ischemic stroke. The invention relates to the field of biomedicine. Background technique [0002] Coronary heart disease, stroke, and vasculitis are very common cardiovascular and cerebrovascular diseases. With the continuous improvement of people's living standards, the incidence of cardiovascular and cerebrovascular diseases is increasing year by year. Risk factors for cardiovascular and cerebrovascular diseases are prevalent, and the prevalence of cardiovascular and cerebrovascular diseases in my country continues to rise. According to statistics, 1 out of every 5 adults suffers from cardiovascular disease. T...

Claims

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Application Information

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IPC IPC(8): C07K7/06C07K1/02A61K38/08A61P9/10
Inventor 赵明彭师奇吴建辉王玉记武丽飞
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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