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Pentamethoxytryptamine carbonylpropionyl-rpak peptide, its preparation, activity and application

A technology of pentamethoxytryptamine and carboxypropionyl, which is applied in the field of biomedicine and can solve problems such as no effective drugs and the like

Active Publication Date: 2019-07-12
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the clinical treatment of ischemic stroke faces the reality that there are no effective drugs, especially for patients with strokes lasting more than 4 hours, either dying or being disabled

Method used

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  • Pentamethoxytryptamine carbonylpropionyl-rpak peptide, its preparation, activity and application
  • Pentamethoxytryptamine carbonylpropionyl-rpak peptide, its preparation, activity and application
  • Pentamethoxytryptamine carbonylpropionyl-rpak peptide, its preparation, activity and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1 connects peptide general method

[0033] Dissolve 1 mmol of the carboxy-terminal compound in dry THF, add 1.2 mmol of N-hydroxybenzotriazole (HOBt) and 1.2 mmol of N, N-dicyclohexylcarbodiimide (DCC) dissolved in dry THF successively under stirring in an ice bath, Stir for 0.5h, dissolve 1.05mmol of the amino-terminal compound in dry THF, add to the above reaction solution, adjust the pH to 9 with N-methylmorpholine (NMM), stir at room temperature for 6h, TLC (CHCl 3 / CH 3 OH, 10 / 1) showed that the carboxy-terminal raw material disappeared completely, and the reaction ended. DCU was removed by filtration, the filtrate was concentrated under reduced pressure and dissolved in ethyl acetate, and the resulting solution was successively washed with saturated NaHCO 3 Wash 3 times with aqueous solution, 3 times with saturated NaCl aqueous solution, 5% KHSO 4 Wash 3 times with aqueous solution, 3 times with saturated NaCl aqueous solution, 5% NaHCO 3 Wash 3 tim...

Embodiment 2

[0034] Embodiment 2 removes N-tert-butoxycarbonyl protecting group general method

[0035] Dissolve 1 mmol of the compound containing N-tert-butoxycarbonyl protecting group in a small amount of dry ethyl acetate, add 10 mL of 4N hydrogen chloride / ethyl acetate solution with stirring in ice bath, stir in ice bath for 1-2 h, TLC (CHCl 3 / CH 3 OH, 10 / 1) showed complete disappearance of the starting material and the reaction was complete. The reaction solution was concentrated under reduced pressure. The residue was added with 5 ml of anhydrous ethyl acetate, and the solution was concentrated to dryness under reduced pressure. This operation was repeated 3 times. The residue was added with 5 ml of anhydrous diethyl ether, and the solution was concentrated to dryness under reduced pressure. This operation was repeated 3 times. The obtained target compound was directly used in the next step reaction.

Embodiment 3

[0036] Embodiment 3 hydrolysis removes benzyl ester protecting group general method

[0037] Dissolve the compound containing the benzyl ester protecting group in methanol, slowly add 2M NaOH aqueous solution dropwise under ice bath and stirring, adjust the pH to 12, react for 5h, TLC (CHCl 3 / CH 3 OH, 10 / 1) showed complete disappearance of the starting material and the reaction was complete. Slowly add saturated KHSO dropwise with stirring in an ice bath 4 The aqueous solution was adjusted to pH 7, concentrated under reduced pressure to remove methanol, and the remaining aqueous solution was slowly added dropwise with saturated KHSO under stirring in an ice bath. 4 The aqueous solution was adjusted to pH 3, extracted 3 times with ethyl acetate, the combined ethyl acetate layer was washed 3 times with saturated NaCl aqueous solution, washed with anhydrous NaCl 2 SO 4 Dry, filter, and concentrate the filtrate under reduced pressure to obtain the target compound.

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Abstract

The invention discloses a pentamethoxytryptophanylcarbonylpropionyl-RPAK peptide, and a preparation method, activities and applications thereof, and concretely relates to a pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val with the formula shown in the description, a preparation method thereof, an antithrombotic activity and a thrombus dissolving activity of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val, and an application of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val in the treatment of stroke rats. The invention also discloses an application of the pentamethoxytryptophanylcarbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val in the preparation of antithrombotic medicines, thrombus dissolving medicines and ischemic stroke treatment medicines.

Description

technical field [0001] The present invention relates to pentamethoxytryptamine carbonylpropionyl-Lys(Arg-Pro-Ala-Lys)-Arg-Gly-Asp-Val, to its preparation method, to its antithrombotic activity, to its thrombolytic effect Activity and its effect on treating ischemic stroke, so the present invention relates to its application in the preparation of antithrombotic drugs, thrombolytic drugs and ischemic stroke drugs. The invention belongs to the field of biomedicine. Background technique [0002] Ischemic stroke is a relatively common and serious cerebrovascular disease, characterized by high incidence, high mortality, high disability rate and high recurrence rate. At present, the clinical treatment of ischemic stroke faces the reality that there is no effective drug, especially for patients with stroke lasting more than 4 hours, either dying or being disabled. It is an important clinical need to invent drugs that are effective for patients with a stroke of more than 4 hours. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06C07K1/06A61K38/08A61P7/02A61P9/10
Inventor 赵明彭师奇吴建辉王玉记傅鸿鸿
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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