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Compound of polyphenols with aza-containing heterocyclic modified and use thereof

A technology of polyphenolic compounds and nitrogen heterocycles is applied in the directions of active ingredients of hydroxy compounds, medical preparations of non-active ingredients, and medical preparations containing active ingredients, etc. very clear etc.

Inactive Publication Date: 2007-07-18
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For many years, the main drug for clinical treatment of this disease is cholinesterase inhibitor, which acts on the cholinergic nervous system and has a relieving effect on the disease, but it cannot prevent the occurrence and development of the disease
At present, the pathogenesis of Alzheimer's disease is not very clear, but it is generally believed that the key cause of the disease is the aggregate (SP) formed by misfolding of excess β-amyloid peptide (Aβ). main component) damages cell membranes, synapses and axons, and causes neurofibrillary tangles

Method used

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  • Compound of polyphenols with aza-containing heterocyclic modified and use thereof
  • Compound of polyphenols with aza-containing heterocyclic modified and use thereof
  • Compound of polyphenols with aza-containing heterocyclic modified and use thereof

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Effect test

Embodiment 1

[0038] Embodiment 1, the preparation of polyphenolic compound

[0039] Synthesizing polyphenolic compound of the present invention, comprises the following steps:

[0040] a. Synthesis of Cyclen-containing monomer [4,7,10-tri-tert-butoxycarbonyl-1,4,7,10-tetraazacyclododecyl-1-yl]acetic acid: Cyclen (purchased from Acros, USA Company) as raw material, first react with Boc20 (di-tert-butyl dicarbonate, purchased from Shanghai Gil Biochemical Company) to obtain 1,4,7-tri-tert-butoxycarbonyl-1,4,7,10-tetraazacyclodeca Second House (3Boc-Cyclen) (see Eiichi Kimura, Shin Aoki, Tohru Koike, and Motoo Shiro, A Tris(ZnII-1, 4, 7, 10-tetraazacyclododecane) Complex as a New Receptor for Phosphate Dianions in Aqueous Solution, Journal of American Chemical Society, 1997, Vol 119, 3068-3076), and then react the product with ethyl bromoacetate (see Joong Won Jeon, Sang Jun Son, Chang Eun Yoo, In Seok Hong, Jung Bae Song, and Junghun Suh, Protein -Cleaving Catalyst Selective for ProteinSub...

Embodiment 2

[0047] Embodiment 2, the preparation of polyphenolic compound

[0048] Synthetic polyphenolic compound of the present invention (molecular formula sees formula VIII), comprises the following steps:

[0049] a. Glycine methyl ester (purchased from Shanghai Jier Biochemical Co., Ltd.) and Cyclen-containing monomer [4,7,10-tri-tert-butoxycarbonyl-1,4,7,10-tetraazacyclic dodecane-1- Base] acetic acid coupling, the connection conditions are in the presence of coupling agents HBTU (purchased from Shanghai Yanchang Biochemical Company), HOBt (purchased from Shanghai Jill Biochemical Company), 1 times the amount of monomer containing Trpn, 1 times the amount of glycine methyl ester, 1 times amount of coupling agent HBTU was reacted with 1 times amount of HOBt at room temperature for 12 hours to obtain a coupled product.

[0050] b. The crude product obtained after the reaction in step a is separated with a silica gel column (column separation condition is: ethyl acetate: petroleum et...

Embodiment 3

[0057] Embodiment 3, the preparation of polyphenolic compound

[0058] Synthetic polyphenolic compound of the present invention (molecular formula sees formula IX), comprises the following steps:

[0059] a. Preparation of Trpn-containing monomer [3(3', 3"-di-tert-butoxycarbonyl-3', 3"-diamino)aminopropylamino]acetic acid: the synthesis method is: Trpn (purchased from the United States Acros Company) as a raw material, first react with Boc20 (di-tert-butyl dicarbonate, purchased from Shanghai Jier Biochemical Company) to obtain 3', 3"-di-tert-butoxycarbonyl-3,3', 3"-triaminopropyl Amine (2Boc-Trpn) (see Eiichi Kimura, Shin Aoki, Tohru Koike, and Motoo Shiro, ATris (ZnII-1, 4, 7, 10-tetraazacyclododecane) Complex as a New Receptor for Phosphate Dianions in Aqueous Solution, Journal of American Chemical Society, 1997, Vol 119, 3068-3076), and then react the product with ethyl bromoacetate (see Joong Won Jeon, Sang Jun Son, Chang Eun Yoo, In Seok Hong, Jung Bae Song, and Junghun...

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Abstract

This invention relates to a nitrogen-containing heterocyclic modified polyphenolic compounds and its applications. Its purpose is to provide a nitrogen-containing heterocyclic modified polyphenolic compounds and applications in the preparation of Alzheimer's disease, Parkinson's disease and other degenerative nervous system disease or type two diabetes preventing and treatment drug. Studies show that the polyphenolic compounds can inhibit aggregation of A beta, also can make the A beta aggregated depolymerize, and will eventually eliminate hydrolysis A beta protein, inhibited and removal of beta A toxicity, in the field of medicine has broad application prospects.

Description

technical field [0001] The present invention relates to polyphenolic compounds and applications thereof, in particular to polyphenolic compounds with nitrogen-containing heterocyclic modifications and their use in the preparation, treatment and prevention of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and type 2 diabetes. application in disease medicine. Background technique [0002] Neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease and type 2 diabetes are protein conformation diseases. Among them, Alzheimer's disease (AD), also known as Alzheimer's disease, is a degenerative disease of the central nervous system, clinically manifested as cognitive impairment, memory loss, and eventually loss of thinking ability, movement disorders, and life. Can not take care of themselves. The pathological features are mainly senile plaque (SP), neurofibrillary tangles (neurofibrillary tangles, NFT) and selective loss of neuro...

Claims

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Application Information

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IPC IPC(8): C07D225/02C07C229/16A61K47/48A61K31/12A61K31/05A61K31/216A61P25/28A61P3/10A61K47/54
Inventor 李艳梅吴为辉雷鹏苏小阳胡笳
Owner TSINGHUA UNIV
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