PAK (polyester alkyd)/ imidazoline/RGD (arginine-glycine-aspartic acid) ternary conjugate and preparation method and use thereof

A technology of tetramethylimidazoline and compounds, which is applied in the field of PAK/imidazoline/RGD ternary conjugates and their preparation and application, can solve the problem of inability to effectively cross the blood-brain barrier, complex and limited curative effect of patients with cerebral infarction to achieve excellent anti-stroke activity, protect neurological function, and reduce the volume of cerebral infarction
CN102887941AInactive Publication Date: 2013-01-23YONG GUANG PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
YONG GUANG PHARMA
Publication Date
2013-01-23
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a PAK(polyester alkyd) / imidazoline / RGD (arginine-glycine-aspartic acid) ternary conjugate and a preparation method and use of the PAK(polyester alkyd) / imidazoline / RGD (arginine-glycine-aspartic acid) ternary conjugate. The method comprises the steps of: taking L-Lys as a connection arm, and connecting 1, 3-dioxy-2-[(4-oxyacetic acid) phenyl]-4, 4, 5, 5-tetramethyl imidazoline, PAK tripeptide with thrombolytic effect, and RGD tetrapeptide with antithrombotic effect together to obtain PAK / imidazoline / RGD ternary complex integrated with three roles of striding blood brain barrier, dissolving thrombus and clearing NO into a whole shown in a formula 1. The PAK / imidazoline / RGD ternary complex disclosed by the invention has high activity of clearing NO free radical, excellent thrombolytic activity and antithrombotic activity. The internal anti-stroke activity proves that the PAK / imidazoline / RGD ternary conjugate can effectively protect a neurologic function of a stroke rat, reduces the cerebral infarction volume of the stoke rat, has the anti-stroke activity, and can be used as a clinical drug for treating cerebral infarction.
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Description

technical field

[0001] The present invention relates to ternary conjugates, in particular to 1-(4-oxoacetyl-phenyl)-3,3,4,4-tetramethyl-imidazoline, PAK tripeptide and RGD tetrapeptide via L- The ternary conjugate obtained by linking Lys together, the present invention also relates to the preparation method of the ternary conjugate, and the present invention further relates to the use of the ternary conjugate in removing NO, antithrombosis, thrombolysis and cerebral infarction treatment The medical use of the invention belongs to the field of PAK / imidazoline / RGD ternary conjugates and their medical use. Background technique

[0002] Globally, thrombotic disease is the leading cause of morbidity and mortality. Coronary thrombosis, leading to myocardial infarction. Cerebrovascular embolism, leading to cerebral infarction. Patients with myocardial infarction can either receive intravenous thrombolytic drugs or undergo bypass surgery. It must be pointed out that the positive...

Claims

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