Hexadecapeptide compound and preparation method and application thereof

A technology of peptide compounds and drugs, which is applied in the field of sixteen peptide compounds and its preparation, can solve the problems of high price and poor safety performance of anti-platelet drugs, and achieve the effects of inhibiting platelet aggregation, low toxicity, and preventing thrombosis

Inactive Publication Date: 2018-09-14
GUANGDONG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the disadvantages or deficiencies of high price and poor safety performance of antiplatelet drugs in the prior art, and provide a hexadecaneptide compound

Method used

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  • Hexadecapeptide compound and preparation method and application thereof
  • Hexadecapeptide compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] This embodiment provides a hexadecanopeptide compound whose polypeptide sequence is RTGACFCVIYNGILYP.

[0038] The sixteen peptide compound can be prepared by the following preparation method:

[0039] Synthesis sequence: from C-terminal to N-terminal.

[0040] (1) Resin swelling: Put 2-Chlorotrityl Chloride Resin into the reaction tube, add DCM (15ml / g), shake for 30min.

[0041] (2) Connect the first amino acid: filter the solvent through the sand core, add amino acid R and 3-fold molar excess (compared with the molar amount of amino acid R) of Fmoc-Pro-OH amino acid, add DMF to dissolve, and then add 10 1-fold molar excess of DIEA (compared to the molar amount of amino acid R), shake for 60 minutes. Block with methanol.

[0042] (3) Deprotection: remove DMF, add 20% piperidine DMF solution (15ml / g) for 5min, remove and add 20% piperidine DMF solution (15ml / g) for 15min.

[0043] (4) Detection: Take out the piperidine solution, take more than a dozen resins, wash ...

Embodiment 2

[0051] This embodiment provides a hexadecaneptide compound, the polypeptide sequence 1 of which is KSGACFCILYQGVVYP.

[0052] The amino acid added in the preparation step of the sixteen peptide compound is inconsistent (the amino acid added is determined according to the type of amino acid in the polypeptide sequence), the rest of the raw materials and steps are consistent with the preparation method provided in Example 1.

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PUM

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Abstract

The invention relates to a hexadecapeptide compound and a preparation method and application thereof. The polypeptide sequence of the hexadecapeptide compound is one or more of RTGACFCVIYNGILYP, or the sequence with the 1-site amino acid R replaced by K, the sequence with the 2-site amino acid T replaced by S, the sequence with the 8-site amino acid V replaced by I or L, the sequence with the 9-site amino acid I replaced by V or L, the sequence with the 11-site amino acid N replaced by Q, the sequence with the 13-site amino acid I replaced by V or L, and the sequence with the 14-site amino acid L replaced by V or I. The hexadecapeptide compound has the functions of prolonging bleeding time, remarkably inhibiting platelet aggregation, and preventing thrombosis, has low toxicity, and has broad application prospects in preparing anti-platelet aggregation or antithrombotic drugs, drug components or prodrugs. The preparation method has high yield and simple process.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a hexadecanopeptide compound and its preparation method and application. Background technique [0002] Thrombotic disease is a kind of disease that seriously affects health, often manifested as myocardial infarction, ischemic cerebral infarction, and venous thromboembolism. At present, the clinical drugs for the treatment of thrombotic diseases are mainly divided into antiplatelet drugs, anticoagulant drugs and thrombolytic drugs. Antiplatelet drugs can inhibit the adhesion, aggregation and release of platelets, thereby preventing thrombus formation. Antiplatelet drugs can effectively prevent the occurrence of cardiovascular diseases and prolong the survival period of patients. Antiplatelet drugs are increasingly widely used in clinical practice. [0003] At present, clopidogrel, which is jointly developed by Bristol-Myers Squibb of the United States and Sanofi-Aventis of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08C07K1/06C07K1/14A61K38/10A61P7/02
CPCA61K38/00A61P7/02C07K7/08
Inventor 张海涛余华军伍俊罗辉
Owner GUANGDONG MEDICAL UNIV
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