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Synthesis, activity and application of dopa-peptide

A compound, -gly-asp technology, applied in the field of biomedicine, can solve problems such as no effective drugs

Active Publication Date: 2020-07-28
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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  • Synthesis, activity and application of dopa-peptide
  • Synthesis, activity and application of dopa-peptide
  • Synthesis, activity and application of dopa-peptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1 prepares (S)-3,4-dihydroxyl-Phe-OBzl

[0021] Stir a solution of 1g (5.08mmol) (S)-3,4-dihydroxy-Phe, 1.02g p-toluenesulfonic acid, 8mL benzyl alcohol and 8mL n-hexane at 90-95°C for 36h, cool to room temperature, pour a large amount of diethyl ether A large amount of colorless solid was precipitated, allowed to stand, and filtered. The filter cake was triturated with ether and dried to give 1.08 g (77%) of the title compound as a yellow powder. ESI-MS(m / z): 288[M+H] + .

Embodiment 2

[0022] Embodiment 2 prepares (S)-3,4-dihydroxyl-Phe(Boc-Ala)-OBzl

[0023] Dissolve 207mg (1.1mmol) Boc-Ala in 15mL of anhydrous tetrahydrofuran (THF), add 149mg (1.1mmol) N-hydroxybenzotriazole (HOBt) and 268mg (1.3mmol) dicyclohexylcarbonyldi The anhydrous THF solution of imine (DCC) was stirred in an ice bath for 20 minutes to obtain the corresponding active ester solution. Dissolve 460mg (1.0mmol) of (S)-3,4-dihydroxy-Phe-OBzl in anhydrous THF, then mix with the newly obtained active ester solution, and add N-methylmorpholine (NMM) dropwise to adjust the pH 8. The resulting reaction mixture was reacted at room temperature for 24 hours. Filtration, the filtrate was concentrated to dryness under reduced pressure, the residue was dissolved in ethyl acetate, and the solution was successively washed with saturated KHSO 4 solution was washed 3 times, saturated NaCl solution was washed 3 times, and the obtained ethyl acetate layer was washed with anhydrous NaCl 2 SO 4 Dry, fi...

Embodiment 3

[0024] Embodiment 3 prepares (S)-3,4-dihydroxyl-Phe(Boc-Ala)

[0025] To 458 mg (1.0 mmol) of (S)-3,4-dihydroxy-Phe(Boc-Ala)-OBzl was added 20 mL of methanol and 30 mg of Pd / C. Pass hydrogen into the obtained suspension, stir at room temperature for 24 hours, TLC (CH 2 Cl 2 / MeOH, 30 / 1) to monitor the disappearance of the reaction raw material point. Pd / C was filtered off, and the filtrate was concentrated under reduced pressure to remove the solvent to obtain 319 mg (86%) of the title compound as a colorless powder. ESI-MS(m / z): 367[M-H] - .

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PUM

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Abstract

The invention discloses 3,4-dyhydroxy-Phe(Ala)-Arg-Gly-Asp-Phe in the formula shown in the specification, a preparation method, anti-thrombus activity of 3,4-dyhydroxy-Phe(Ala)-Arg-Gly-Asp-Phe, and an effect of 3,4-dyhydroxy-Phe(Ala)-Arg-Gly-Asp-Phe on the treatment of cerebral ischemia mices, so that the invention discloses application of 3,4-dyhydroxy-Phe(Ala)-Arg-Gly-Asp-Phe in preparation of anti-thrombus drugs and ischemic stroke treatment drugs.

Description

technical field [0001] The present invention relates to 3,4-dihydroxy-Phe(Ala)-Arg-Gly-Asp-Phe, to its preparation method, to its antithrombotic activity, to its thrombolytic activity, to its treatment of cerebral ischemia Therefore, the present invention relates to its application in the preparation of antithrombotic drugs, thrombolytic drugs and drugs for treating ischemic stroke. 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. The inventor once disclosed th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06A61K38/08A61P7/02A61P9/10
Inventor 彭师奇赵明王夏
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES