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PAK-tetramethyl-1,3-dioxoimidazoline as well as synthesis, activity and application thereof

A dioxyimidazoline, tetramethyl technology, applied in the direction of tetrapeptide components, drug combinations, blood diseases, etc., can solve problems such as no effective drugs

Inactive Publication Date: 2017-01-11
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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  • PAK-tetramethyl-1,3-dioxoimidazoline as well as synthesis, activity and application thereof
  • PAK-tetramethyl-1,3-dioxoimidazoline as well as synthesis, activity and application thereof
  • PAK-tetramethyl-1,3-dioxoimidazoline as well as synthesis, activity and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 prepares 2,3-dimethyl-2,3-dinitrobutane

[0024] Add 130mL of 6N NaOH solution successively to 69.0g (0.78mol, 70mL) of 2-nitropropane under ice bath and stirring, 20mL (0.38mol, slowly dropwise, within 1 hour) of Br 2 and 240 mL of ethanol. The reaction mixture was refluxed at 90°C for 3 hours, during which a flake precipitate appeared. The reaction solution was poured into 800 mL of ice water while hot, and 49.0 g (73%) of the title compound was obtained by filtration as colorless flaky crystals. ESI-MS(m / e): 177[M+H] + .

Embodiment 2

[0025] Embodiment 2 prepares 2,3-dimethyl-2,3-dihydroxyaminobutane

[0026] 7.00g (40mmol) 2,3-dimethyl-2,3-dinitrobutane and 4.00g NH 4 Cl was dissolved in 80mL of 50% ethanol water[]\solution, stirred under ice bath, and 16.00g of zinc powder was added in batches within 3 hours. After the zinc powder was added, the reaction mixture was stirred at room temperature for 3 h, filtered with suction, and the filter cake was repeatedly washed with 50% aqueous ethanol. Combine the filtrate and washing liquid, adjust the pH to 2 with concentrated hydrochloric acid, and concentrate under reduced pressure to obtain a slurry. Dissolve the slurry with a small amount of 50% ethanol aqueous solution, add an appropriate amount of potassium carbonate, mix well, put it into a Soxhlet extractor, use dichloromethane as the extractant, extract at 60°C for 6 hours, concentrate the extract under reduced pressure, and use the residue Trituration with petroleum ether gave 2.07 g (35%) of the title...

Embodiment 3

[0027] Example 3 Preparation of 2-(3-carboxy-4-hydroxyphenyl)-1,3-dihydroxy-4,4,5,5-tetramethylimidazole

[0028] Dissolve 1.48g (10mmol) of 2,3-dimethyl-2,3-dihydroxyaminobutane in a small amount of methanol at room temperature, add 2.0g (12mmol) of 3-carboxy-4-hydroxybenzaldehyde, and react for 12 hours. Filtration afforded 2.07 g (70%) of the title compound as a colorless powder. ESI-MS(m / e): 298[M+H] + .

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PUM

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Abstract

The invention discloses PAK-tetramethyl-1,3-dioxoimidazoline of a formula I as shown in the specification, a preparation method thereof, activity thereof in scavenging free radicals, antithrombotic activity thereof, thrombolytic activity thereof, and a function thereof in treating stroke rats, therefore, the invention discloses applications of the PAK-tetramethyl-1,3-dioxoimidazoline in preparing a medicine for scavenging the free radicals, an antithrombotic medicine, a thrombolytic medicine and a medicine for treating ischemic stroke.

Description

technical field [0001] The present invention relates to 2-[3-(formyl-Pro-Ala-Lys)-4-(oxyacetyl-Arg-Gly-Asp-AA)]phenyl-4,4,5,5-tetramethyl-1 , 3-dioximidazolines, relate to their preparation method, relate to their activity of scavenging free radicals, relate to their antithrombotic activity, relate to their thrombolytic activity and relate to their effect of treating ischemic stroke, thus the present invention relates to Their application in the preparation of free radical scavenging drugs, antithrombotic drugs, thrombolytic drugs and ischemic stroke drugs. 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 cl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/11C07K1/06A61K38/07A61P39/06A61P7/02A61P9/10
Inventor 赵明彭师奇吴建辉王玉记李聪颖
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES